Ko 143

目录号: HY-10010 纯度: 99.97%: FAQs
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摩尔计算器

Ko 143 是有效且选择性的 ATP 结合盒亚家族 G 成员 2 (ABCG2/BCRP) 抑制剂。Ko 143 比 P-gp 和 MRP-1 运输蛋白高出 200 倍的选择性。

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Ko 143 Chemical Structure

CAS No. : 461054-93-3

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10 mM * 1 mL in DMSO	￥980	In-stock
1 mg	￥431	In-stock
5 mg	￥949	In-stock
10 mg	￥1525	In-stock
25 mg	￥3600	In-stock
50 mg	￥5488	In-stock
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Customer Review

MCE 顾客使用本产品发表的 36 篇科研文献

Proliferation Assay

: Ko 143 purchased from MCE. Usage Cited in: Drug Deliv. 2017 Nov;24(1):1453-1459. [Abstract]; Fluorescent substrates accumulate in the organoids. The organoids are incubated in Hoechst 33342 with or without YHO-13177 or Ko143 for 20, 60 and 100 minutes, respectively. Ko143 and YHO-13177 notably decrease the fluorescence intensity of Hoechst 33342 in the organoids.

: Ko 143 purchased from MCE. Usage Cited in: J Drug Target. 2016;24(5):441-9. [Abstract]; Cells are co-treated with 5 μM of free LY156758 or an equivalent dose of SMA-LY156758 and either vehicle control (0.01% DMSO), Elacridar (1 μM), KO143 (5 μM), Valspodar (1 μM) or a combination of efflux inhibitors for 6 h.

: Ko 143 purchased from MCE. Usage Cited in: J Pharm Biomed Anal. 2012 Jul;66:232-9. [Abstract]; Effect of pharmacological inhibition of drug efflux transporters on brain distribution of FLZ in rats. The rats receive 35 mg/kg FLZ via tail vein injection 10 min after intravenous administration of 20 mg/kg Zosuquidar or 7.5 mg/kg ko143.

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Ko 143 is a potent and selective ATP-binding cassette subfamily G member 2 (ABCG2/BCRP) inhibitor. Ko 143 displays >200-fold selectivity over P-gp and MRP-1 transporters^[1]^[2].

IC₅₀ & Target

EC90: 26 nM (BCRP)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	122.83 nM Compound: Ko143	Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 1625.4 +/-413.42 nM) Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 1625.4 +/-413.42 nM)	[PMID: 34496204]
A549	IC₅₀	127.7 nM Compound: Ko143	Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 1162.92 +/-250.73 nM) Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 1162.92 +/-250.73 nM)	[PMID: 34496204]
A549	IC₅₀	236.09 nM Compound: Ko143	Chemo-sensitizing activity against human A549 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 376.13 +/-60.17 nM) Chemo-sensitizing activity against human A549 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 376.13 +/-60.17 nM)	[PMID: 34496204]
A549	IC₅₀	326.96 nM Compound: Ko143	Chemo-sensitizing activity against human A549 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb =555.44 +/-125.7 nM) Chemo-sensitizing activity against human A549 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb =555.44 +/-125.7 nM)	[PMID: 34496204]
A549	IC₅₀	37.17 nM Compound: Ko143	Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 552.97 +/-106.74 nM) Chemo-sensitizing activity against becatecarin-selected ABCG2-overexpressing human A549/Bec150 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 552.97 +/-106.74 nM)	[PMID: 34496204]
A549	IC₅₀	41.83 nM Compound: Ko143	Chemo-sensitizing activity against human A549 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 82.47 +/-24.25 nM) Chemo-sensitizing activity against human A549 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 82.47 +/-24.25 nM)	[PMID: 34496204]
Caco-2	IC₅₀	> 30 μM Compound: Ko143	Inhibition of P-gp transporter in human Caco2 cells using [3H]-digoxin as substrate measured at 30 to 120 mins by microplate scintillation and luminescence counting analysis Inhibition of P-gp transporter in human Caco2 cells using [3H]-digoxin as substrate measured at 30 to 120 mins by microplate scintillation and luminescence counting analysis	[PMID: 26642765]
HEK293	EC₅₀	0.012 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux at 5 uM after 30 mins in presence of 0.1 uM (2E,2'E)-1,1'-(1,4-Phenylene)bis(3-(2,6-dimethoxyphenyl)-prop-2-en-1-one) by flow cytometry Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux at 5 uM after 30 mins in presence of 0.1 uM (2E,2'E)-1,1'-(1,4-Phenylene)bis(3-(2,6-dimethoxyphenyl)-prop-2-en-1-one) by flow cytometry	[PMID: 24611893]
HEK293	EC₅₀	0.029 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux after 30 mins by flow cytometry relative to control Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux after 30 mins by flow cytometry relative to control	[PMID: 24611893]
HEK293	IC₅₀	0.05 μM Compound: Ko143	Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry	[PMID: 22165858]
HEK293	EC₅₀	0.074 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by flow cytometric analysis Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by flow cytometric analysis	[PMID: 27376492]
HEK293	IC₅₀	0.09 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by FACS method Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by FACS method	[PMID: 25272055]
HEK293	EC₅₀	0.09 μM Compound: Ko143	Inhibition of ABCG2 (unknown origin)-mediated mitoxantrone efflux expressed in HEK293 cells after 30 mins by flow cytometric analysis Inhibition of ABCG2 (unknown origin)-mediated mitoxantrone efflux expressed in HEK293 cells after 30 mins by flow cytometric analysis	[PMID: 24304387]
HEK293	IC₅₀	2.53 nM Compound: Ko143	Chemo-sensitizing activity against human HEK293 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 2.74 +/-0.69 nM) Chemo-sensitizing activity against human HEK293 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 2.74 +/-0.69 nM)	[PMID: 34496204]
HEK293	IC₅₀	2.69 nM Compound: Ko143	Chemo-sensitizing activity against human HEK293 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 2.78 +/-0.58 nM) Chemo-sensitizing activity against human HEK293 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 2.78 +/-0.58 nM)	[PMID: 34496204]
HEK293	IC₅₀	38.59 nM Compound: Ko143	Chemo-sensitizing activity against human HEK293 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 35.17 +/-8.65 nM) Chemo-sensitizing activity against human HEK293 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 35.17 +/-8.65 nM)	[PMID: 34496204]
HEK293	IC₅₀	8.36 nM Compound: Ko143	Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 99.55 +/-7.35 nM) Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 99.55 +/-7.35 nM)	[PMID: 34496204]
HEK293	IC₅₀	9.94 nM Compound: Ko143	Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 239.91 +/-25 nM) Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 239.91 +/-25 nM)	[PMID: 34496204]
HEK293	IC₅₀	96.43 nM Compound: Ko143	Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 558.68 +/-81.31 nM) Chemo-sensitizing activity against ABCG2-overexpressing human HEK293/482R cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 558.68 +/-81.31 nM)	[PMID: 34496204]
K562	IC₅₀	71.53 μM Compound: Ko143	Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay Cytotoxicity against human K562 cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
K562/A02	IC₅₀	58.74 μM Compound: Ko143	Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay Cytotoxicity against P-gp overexpressing human K562/A02 cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
MCF7	IC₅₀	0.23 μM Compound: Ko143	Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining	[PMID: 19932960]
MCF7	IC₅₀	0.39 μM Compound: Ko143	Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining Inhibition of BCRP expressed in MCF-7 MX cells using Hoechst 33342 staining	[PMID: 21354800]
MDCK	IC₅₀	> 50000 nM Compound: 2, Ko143	Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay Inhibition of ABCC2 overexpressed in MDCK cells at 100 uM by flow cytometric-based chloromethylfluorescein-diacetate accumulation assay	[PMID: 19170519]
MDCK	IC₅₀	0.074 μM Compound: Ko143	Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay	[PMID: 19932960]
MDCK	IC₅₀	0.21 μM Compound: Ko143	Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining Inhibition of BCRP expressed in MDCK cells using Hoechst 33342 staining	[PMID: 21354800]
MDCK	IC₅₀	93.27 μM Compound: Ko143	Cytotoxicity against dog MDCK cells after 48 hrs by MTT assay Cytotoxicity against dog MDCK cells after 48 hrs by MTT assay	[PMID: 35247755]
MDCK-II	IC₅₀	0.128 μM Compound: Ko143	Inhibition of GFP-tagged human BCRP expressed in MDCK2 cells pre-incubated for 30 mins followed by Hoechst 33342 addition and further incubated for 120 mins by Hoechst 33342 accumulation assay Inhibition of GFP-tagged human BCRP expressed in MDCK2 cells pre-incubated for 30 mins followed by Hoechst 33342 addition and further incubated for 120 mins by Hoechst 33342 accumulation assay	[PMID: 25855895]
MDCK-II	IC₅₀	0.215 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of Hoechst 33342 preincubated for 30 mins before Hoechst 33342 addition measured after 120 mins by fluorescence assay	[PMID: 23851114]
MDCK-II	IC₅₀	0.221 μM Compound: Ko143	Inhibition of recombinant human GFP-fused ABCG2 expressed in MDCK2 cells assessed as reduction in Hoechst 33342 efflux preincubated for 30 mins followed by Hoechst 33342 addition measured immediately at 60 sec time interval for 120 mins by fluorescence as Inhibition of recombinant human GFP-fused ABCG2 expressed in MDCK2 cells assessed as reduction in Hoechst 33342 efflux preincubated for 30 mins followed by Hoechst 33342 addition measured immediately at 60 sec time interval for 120 mins by fluorescence as	[PMID: 27676469]
MDCK-II	IC₅₀	0.24 μM Compound: Ko143	Inhibition of human C-terminal GFP-tagged ABCG2 expressed in MDCK2 cells using pheophorbide A as substrate preincubated for 20 mins followed by substrate addition measured after 120 mins by flow cytometry Inhibition of human C-terminal GFP-tagged ABCG2 expressed in MDCK2 cells using pheophorbide A as substrate preincubated for 20 mins followed by substrate addition measured after 120 mins by flow cytometry	[PMID: 27100033]
MDCK-II	IC₅₀	0.25 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation treated 30 mins before Hoechst 33342 addition measured up to 120 mins by fluorescence assay	[PMID: 24184213]
MDCK-II	IC₅₀	0.25 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells preincubated for 30 mins prior to Hoechst 33342 addition measured every 60 secs up to 120 mins by Hoechst 33342 accumulation assay Inhibition of human BCRP expressed in MDCK2 cells preincubated for 30 mins prior to Hoechst 33342 addition measured every 60 secs up to 120 mins by Hoechst 33342 accumulation assay	[PMID: 23017888]
MDCK-II	IC₅₀	0.26 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation preincubated for 30 mins by fluorimetry Inhibition of human BCRP expressed in MDCK2 cells assessed as Hoechst 33342 accumulation preincubated for 30 mins by fluorimetry	[PMID: 22112540]
MDCK-II	IC₅₀	0.276 μM Compound: Ko143	Inhibition of recombinant human GFP-fused ABCG2 expressed in MDCK2 cells assessed as reduction in pheophorbide A efflux preincubated for 30 mins followed by pheophorbide A addition measured after 2 hrs by flow cytometry Inhibition of recombinant human GFP-fused ABCG2 expressed in MDCK2 cells assessed as reduction in pheophorbide A efflux preincubated for 30 mins followed by pheophorbide A addition measured after 2 hrs by flow cytometry	[PMID: 27676469]
MDCK-II	IC₅₀	0.33 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as pheophorbide A accumulation treated 30 mins before pheophorbide A addition measured up to 120 mins by flow cytometry Inhibition of human BCRP expressed in MDCK2 cells assessed as pheophorbide A accumulation treated 30 mins before pheophorbide A addition measured up to 120 mins by flow cytometry	[PMID: 24184213]
MDCK-II	IC₅₀	0.354 μM Compound: Ko143	Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry Inhibition of human BCRP expressed in MDCK2 cells assessed as accumulation of pheophorbide-A preincubated for 30 mins before pheophorbide-A addition measured after 120 mins by flow cytometry	[PMID: 23851114]
MDCK-II	GI₅₀	10.9 μM Compound: Ko143	Cytotoxicity against wild-type MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against wild-type MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27280693]
MDCK-II	GI₅₀	10.9 μM Compound: Ko143	Intrinsic cytotoxicity against parental MDCK2 cells incubated for 72 hrs by MTT assay Intrinsic cytotoxicity against parental MDCK2 cells incubated for 72 hrs by MTT assay	[PMID: 27148793]
MDCK-II	GI₅₀	10.9 μM Compound: Ko143	Cytotoxicity against MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
MDCK-II	GI₅₀	11.1 μM Compound: Ko143	Cytotoxicity against MDCK2 cells expressing human ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells expressing human ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27280693]
MDCK-II	GI₅₀	11.1 μM Compound: Ko143	Intrinsic cytotoxicity against MDCK2 cells over-expressing human ABCG2 incubated for 72 hrs by MTT assay Intrinsic cytotoxicity against MDCK2 cells over-expressing human ABCG2 incubated for 72 hrs by MTT assay	[PMID: 27148793]
MDCK-II	GI₅₀	11.1 μM Compound: Ko143	Cytotoxicity against MDCK2 cells expressing human C-terminal GFP-tagged ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells expressing human C-terminal GFP-tagged ABCG2 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
MDCK-II	GI₅₀	12.5 μM Compound: Ko143	Growth inhibition of MDCK2 cells after 72 hrs by MTT assay Growth inhibition of MDCK2 cells after 72 hrs by MTT assay	[PMID: 30390439]
MDCK-II	GI₅₀	12.5 μM Compound: 59; Ko143	Intrinsic cytotoxicity in parental MDCK2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Intrinsic cytotoxicity in parental MDCK2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 30075623]
MDCK-II	GI₅₀	12.5 μM Compound: Ko143	Cytotoxicity against MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 28841513]
MDCK-II	GI₅₀	12.5 μM Compound: 55; Ko143	Cytotoxicity against MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 28471656]
MDCK-II	GI₅₀	12.6 μM Compound: Ko143	Growth inhibition of MDCK2 cells harboring GFP-fused human ABCG2 after 72 hrs by MTT assay Growth inhibition of MDCK2 cells harboring GFP-fused human ABCG2 after 72 hrs by MTT assay	[PMID: 30390439]
MDCK-II	GI₅₀	12.6 μM Compound: 59; Ko143	Intrinsic cytotoxicity in MDCK2 cells overexpressing BCRP assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Intrinsic cytotoxicity in MDCK2 cells overexpressing BCRP assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 30075623]
MDCK-II	GI₅₀	12.6 μM Compound: Ko143	Cytotoxicity against MDCK2 cells harboring human ABCG2 assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells harboring human ABCG2 assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 28841513]
MDCK-II	GI₅₀	12.6 μM Compound: 55; Ko143	Cytotoxicity against ABCG2 over-expressing MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against ABCG2 over-expressing MDCK2 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 28471656]
MDCK-II	GI₅₀	13 μM Compound: 56; Ko143	Cytotoxicity against MDCK2 cells expressing human BCRP assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells expressing human BCRP assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 29547272]
MDCK-II	GI₅₀	13 μM Compound: 56; Ko143	Cytotoxicity against MDCK2 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against MDCK2 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 29547272]
MDCK-II	IC₅₀	58.26 μM Compound: Ko143	Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay Cytotoxicity against BCRP-overexpressing MDCK-II cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
MDCK-II	IC₅₀	87.19 μM Compound: Ko143	Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay Cytotoxicity against MDCK-II cells incubated for 48 hrs by MTT assay	[PMID: 33938746]
NCI-H460	IC₅₀	0.21 μM Compound: Ko143	Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 4.33 +/-1.18 microM) Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 4.33 +/-1.18 microM)	[PMID: 34496204]
NCI-H460	IC₅₀	102.95 nM Compound: Ko143	Chemo-sensitizing activity against human NCI-H460 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 279.69 +/-31.94 nM) Chemo-sensitizing activity against human NCI-H460 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 279.69 +/-31.94 nM)	[PMID: 34496204]
NCI-H460	IC₅₀	12.27 nM Compound: Ko143	Chemo-sensitizing activity against human NCI-H460 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 20.7 +/-6.32 nM) Chemo-sensitizing activity against human NCI-H460 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 20.7 +/-6.32 nM)	[PMID: 34496204]
NCI-H460	IC₅₀	144.61 nM Compound: Ko143	Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 3262.6 +/-811.81 nM) Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as topotecan IC50 at 1 uM measured after 72 hrs in presence of topotecan by CCK8 assay (Rvb = 3262.6 +/-811.81 nM)	[PMID: 34496204]
NCI-H460	IC₅₀	42.61 nM Compound: Ko143	Chemo-sensitizing activity against human NCI-H460 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 128.27 +/-22.6 nM) Chemo-sensitizing activity against human NCI-H460 cells assessed as SN-38 IC50 at 1 uM measured after 72 hrs in presence of SN-38 by CCK8 assay (Rvb = 128.27 +/-22.6 nM)	[PMID: 34496204]
NCI-H460	IC₅₀	53.43 nM Compound: Ko143	Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 963.32 +/-120.89 nM) Chemo-sensitizing activity against mitoxantrone-selected ABCG2-overexpressing human NCI-H460/MX20 cells assessed as mitoxantrone IC50 at 1 uM measured after 72 hrs in presence of mitoxantrone by CCK8 assay (Rvb = 963.32 +/-120.89 nM)	[PMID: 34496204]
Sf9	IC₅₀	0.004 μM Compound: Ko143	Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive basal ATPase activity after 20 mins by colorimetric method Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive basal ATPase activity after 20 mins by colorimetric method	[PMID: 27280693]
Sf9	IC₅₀	0.028 μM Compound: Ko143	Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive quercetin-stimulated ATPase activity after 20 mins by colorimetric method Inhibition of human ABCG2 expressed in baculovirus infected Sf9 cell membrane assessed as inhibition of vanadate sensitive quercetin-stimulated ATPase activity after 20 mins by colorimetric method	[PMID: 27280693]
Sf9	IC₅₀	0.17 μM Compound: Ko143	Inhibition of human ABCG2 expressed in Sf9 insect cell membranes assessed as inhibition of quercetin-stimulated ATPase activity after 30 mins by colorimetric analysis in presence of sodium orthovanadate Inhibition of human ABCG2 expressed in Sf9 insect cell membranes assessed as inhibition of quercetin-stimulated ATPase activity after 30 mins by colorimetric analysis in presence of sodium orthovanadate	[PMID: 24304387]

体外研究
(In Vitro)

Ko143 (10 nM) 显著降低 (2.5 倍) MTX 对 HEK G2 细胞和小鼠 G2 细胞的 IC₅₀。Ko143 (1-100 μM) 代谢物不抑制 ABC 转运蛋白的功能^[1]。
FTC 类似物 Ko143 逆转 SKF 104864A 选择的小鼠 MEF3.8/T6400 细胞和人 IGROV1/T8 细胞的耐药性。Ko143 的应用浓度为 EC₉₀ 25 nM 的零、一或八倍^[2]。
Ko143 抑制 Madin-Darby 犬肾 (MDCK) 2-BCRP421CC (野生型) 细胞和 MDCK2-BCRP421AA (突变型) 细胞中 BCRP 介导的 ZD 4522 转运^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Ko143 (10 mg/kg，口服) 增加小鼠体内 SKF 104864A 的口服利用度^[2]。
Ko143 显著影响 ZD 4522 在大鼠体内的药代动力学^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

469.57

Formula

C₂₆H₃₅N₃O₅

CAS 号

461054-93-3

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (212.96 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1296 mL	10.6480 mL	21.2961 mL
5 mM	0.4259 mL	2.1296 mL	4.2592 mL
10 mM	0.2130 mL	1.0648 mL	2.1296 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.32 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.32 mM); 悬浊液; 超声助溶 (<50°C)

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.32 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案四

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (5.32 mM); 悬浊液; 超声助溶

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.97%

选择批次：

Data Sheet (640 KB) SDS (393 KB)

COA (263 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Weidner LD, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93. [Content Brief]

[2]. JD Allen et al. Potent and Specific Inhibition of the Breast Cancer Resistance Protein Multidrug Transporter in Vitro and in Mouse Intestine by a Novel Analogue of Fumitremorgin C. Mol. Cancer Ther. 2002, 1, 417-425. [Content Brief]

[3]. Wen JH, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of ZD 4522 In Vivo and Vitro. Chin Med Sci J. 2015 Dec;30(4):218-25. [Content Brief]

[4]. Hou J, et al. Quantitative determination and pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:232-9. [Content Brief]

[5]. Liu K, et al. Metabolism of KO143, an ABCG2 inhibitor. Drug Metab Pharmacokinet. 2017 Aug;32(4):193-200. [Content Brief]

Cell Assay ^[2]	cells are plated at 400 or 1000/well in 96-well plates the night before addition of drugs. A concentration series of drug is applied along one plate axis and left for the duration of the assay. Plates are harvested after 4-5 days while untreated wells are still subconfluent. Relative cell proliferation is quantified with CyQuant or Sybr Green I fluorescent nucleic acid stains. Assays with human cell lines are performed in the presence of 0.1 μm PSC833 to inhibit confounding P-gp activity. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Oral toxicity of FTC analogues in mice is tested by mixing 50 mg/mL stocks in DMSO 1:1 with Tween 80 (polyoxyethylene sorbitan mono-oleate) and diluting with 5% w/v glucose such that the final volume administered by oral gavage is 10 μL/g of body weight. Pairs of mice are administered oral doses of 50 mg/kg Ko132, Ko134, Ko143, or vehicle under light methoxyflurane anesthesia. Final tests of 50 mg/kg Ko134 or Ko143 are performed on additional pairs of unanesthetized animals to observe any behavioral effects. Further, another pair of mice receive the higher dose of 100 mg/kg Ko134. For i.p. toxicity tests, the FTC analogue stocks in DMSO are dispersed in at least 10 volumes of sterile corn oil such that the injected volume is 5 μL/g of body weight. After pilot tests at lower doses show no adverse effects, mice (4 per group) are administered vehicle or 10 mg/kg i.p. of Ko132, Ko134, or Ko143. The mice are observed continuously during the first hour after administration and then at increasing intervals for 2 weeks, after which they are sacrificed for histological examination of major organs and structures including brain, salivary glands, heart, lungs, liver, adrenal glands, kidneys, urinary tract, spleen, thymus, bone marrow, pancreas, stomach, intestines, cecum, colon, testes, epididymus, skin, head, trunk, and limbs. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Weidner LD, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93. [Content Brief] [2]. JD Allen et al. Potent and Specific Inhibition of the Breast Cancer Resistance Protein Multidrug Transporter in Vitro and in Mouse Intestine by a Novel Analogue of Fumitremorgin C. Mol. Cancer Ther. 2002, 1, 417-425. [Content Brief] [3]. Wen JH, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of ZD 4522 In Vivo and Vitro. Chin Med Sci J. 2015 Dec;30(4):218-25. [Content Brief] [4]. Hou J, et al. Quantitative determination and pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:232-9. [Content Brief] [5]. Liu K, et al. Metabolism of KO143, an ABCG2 inhibitor. Drug Metab Pharmacokinet. 2017 Aug;32(4):193-200. [Content Brief]

Ko 143 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1296 mL	10.6480 mL	21.2961 mL	53.2402 mL
	5 mM	0.4259 mL	2.1296 mL	4.2592 mL	10.6480 mL
	10 mM	0.2130 mL	1.0648 mL	2.1296 mL	5.3240 mL
	15 mM	0.1420 mL	0.7099 mL	1.4197 mL	3.5493 mL
	20 mM	0.1065 mL	0.5324 mL	1.0648 mL	2.6620 mL
	25 mM	0.0852 mL	0.4259 mL	0.8518 mL	2.1296 mL
	30 mM	0.0710 mL	0.3549 mL	0.7099 mL	1.7747 mL
	40 mM	0.0532 mL	0.2662 mL	0.5324 mL	1.3310 mL
	50 mM	0.0426 mL	0.2130 mL	0.4259 mL	1.0648 mL
	60 mM	0.0355 mL	0.1775 mL	0.3549 mL	0.8873 mL
	80 mM	0.0266 mL	0.1331 mL	0.2662 mL	0.6655 mL
	100 mM	0.0213 mL	0.1065 mL	0.2130 mL	0.5324 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ko 143461054-93-3Ko143Ko-143BCRPBreast cancer resistance proteinABCG2Inhibitorinhibitorinhibit

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