Rociletinib (Synonyms: CO-1686; AVL-301; CNX-419)

目录号: HY-15729 纯度: 99.79%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

Rociletinib (CO-1686) 是一种可口服的 EGFR 抑制剂，能够抑制 EGFRL858R/T790M 和 EGFRWT 的活性，IC₅₀ 值分别为 21.5 nM 和 303.3 nM。

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Rociletinib Chemical Structure

CAS No. : 1374640-70-6

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥611	In-stock
5 mg	￥500	In-stock
10 mg	￥800	In-stock
50 mg	￥1500	In-stock
100 mg	￥2500	In-stock
200 mg		询价
500 mg		询价

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Customer Review

Other Forms of Rociletinib:

Rociletinib hydrobromide In-stock

MCE 顾客使用本产品发表的 13 篇科研文献

RT-PCR

: Rociletinib purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811. [Abstract]; The protein level of ABCG2 on MDR cells after 0, 0.25, 0.5 and 1 µmol/L rociletinib stimulation for 48 h are measured by Western blot analysis.

: Rociletinib purchased from MCE. Usage Cited in: Acta Pharm Sin B. 2020 May;10(5):799-811. [Abstract]; Rociletinib enhances the anticancer effect of topotecan in the S1-MI-80 tumor xenograft model in nude mice. (A)The changes in tumor volume over time after the S1-MI-80 cell implantation (n=6). Data shown are mean±SD of tumor volumes for each group. (B) The image of tumors size in four groups excised from the mice on the 75th day after implantation.

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Rociletinib (CO-1686) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the K_i values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively.

IC₅₀ & Target^[1]

EGFR^L858R/T790M

21.5 nM (Ki)

EGFR^T790M

303.3 nM (Ki)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A-431	IC₅₀	> 4331 nM Compound: CO-1686	Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysis Inhibition of wild type EGFR phosphorylation in human A431 cells after 1 hr by Western blot analysis	[PMID: 26968253]
A-431	IC₅₀	1.29 μM Compound: 4	Antiproliferative activity against wild type human A431 cells after 48 hrs by MTT assay Antiproliferative activity against wild type human A431 cells after 48 hrs by MTT assay	[PMID: 27634676]
A-431	IC₅₀	1.29 μM Compound: Rociletinib	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
A-431	IC₅₀	1.545 μM Compound: 2	Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay	[PMID: 28033579]
A-431	EC₅₀	1.66 μM Compound: Rociletinib	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A-431	IC₅₀	1.79 μM Compound: Rociletinib	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
A-431	IC₅₀	1.794 μM Compound: 5	Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A431 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
A-431	GI₅₀	547 nM Compound: CO-1686	Antiproliferative activity against wild type EGFR expressing human A431 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against wild type EGFR expressing human A431 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
A-431	IC₅₀	6.01 μM Compound: Rociletinib	Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
A-431	IC₅₀	641 nM Compound: 5; CO-1686	Cytotoxicity against human A431 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by SRB assay Cytotoxicity against human A431 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by SRB assay	[PMID: 29906114]
A549	IC₅₀	1600 nM Compound: 8; CO-1686	Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA	[PMID: 26756222]
A549	IC₅₀	3.24 μM Compound: Rociletinib	Antiproliferative activity against human A549 cells harboring EGFR K-ras mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells harboring EGFR K-ras mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
A549	IC₅₀	3.242 μM Compound: 5	Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
A549	IC₅₀	6.5 μM Compound: Rociletinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
A549	IC₅₀	6.502 μM Compound: 4	Antiproliferative activity against human A549 cells harboring K-ras mutation after 48 hrs by MTT assay Antiproliferative activity against human A549 cells harboring K-ras mutation after 48 hrs by MTT assay	[PMID: 27634676]
A549	IC₅₀	7.57 μM Compound: CO-1686	Anti-proliferative activity against human A549 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human A549 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
BaF3	GI₅₀	0.94 μM Compound: 4; C01686	Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay	[PMID: 28282122]
COS-7	IC₅₀	7.39 μM Compound: Rociletinib	Cytotoxicity against African green monkey COS7 cells assessed as decrease in cell viability incubated incubated for 48 hrs by MTT assay Cytotoxicity against African green monkey COS7 cells assessed as decrease in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
HaCaT	IC₅₀	262.3 nM Compound: 6; CO-1686	Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method	[PMID: 27433829]
HCC827	GI₅₀	0.03 μM Compound: CO-1686	Growth inhibition of human HCC827 cells with exon 19 deletion and delE746-A750 incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human HCC827 cells with exon 19 deletion and delE746-A750 incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
HCC827	IC₅₀	0.031 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
HCC827	IC₅₀	0.031 μM Compound: 5	Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
HCC827	IC₅₀	0.031 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells harboring EGFR del E746 to A750 mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCC827 cells harboring EGFR del E746 to A750 mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
HCC827	EC₅₀	0.045 μM Compound: Rociletinib	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCC827	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR Del 19 mutant expressing human HCC827 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR Del 19 mutant expressing human HCC827 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
NCI-H1975	GI₅₀	0.03 μM Compound: CO-1686	Growth inhibition of human NCI-H1975 cells expressing EGFR L858R/T790M mutant incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human NCI-H1975 cells expressing EGFR L858R/T790M mutant incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
NCI-H1975	IC₅₀	0.042 μM Compound: 2	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 28033579]
NCI-H1975	EC₅₀	0.1 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H1975	IC₅₀	0.13 μM Compound: CO-1686	Anti-proliferative activity against human NCI-H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human NCI-H1975 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
NCI-H1975	IC₅₀	0.137 μM Compound: 4	Antiproliferative activity against human NCI-H1975 cells harboring L858R/T790M double mutant after 48 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring L858R/T790M double mutant after 48 hrs by MTT assay	[PMID: 27634676]
NCI-H1975	IC₅₀	0.137 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
NCI-H1975	IC₅₀	0.137 μM Compound: Rociletinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as decrease in cell viability after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28385595]
NCI-H1975	IC₅₀	0.299 μM Compound: 5	Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay	[PMID: 28395219]
NCI-H1975	IC₅₀	0.51 μM Compound: Rociletinib	Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
NCI-H1975	IC₅₀	16 nM Compound: 8; CO-1686	Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
NCI-H1975	IC₅₀	31 nM Compound: 5; CO-1686	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay	[PMID: 29906114]
NCI-H1975	IC₅₀	62 nM Compound: CO-1686	Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysis Inhibition of EGFR L858R / T790M double mutant phosphorylation in human NCI-H1975 cells after 1 hr by Western blot analysis	[PMID: 26968253]
NCI-H1975	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR L858R / T790M double mutant expressing human NCI-H1975 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR L858R / T790M double mutant expressing human NCI-H1975 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
NCI-H358	IC₅₀	> 2000 nM Compound: CO-1686	Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysis Inhibition of wild type EGFR phosphorylation in human NCI-H358 cells after 1 hr by Western blot analysis	[PMID: 26968253]
NCI-H661	GI₅₀	1.7 μM Compound: CO-1686	Growth inhibition of human NCI-H661 cells incubated for 96 hrs by cell-titer Glo reagent based assay Growth inhibition of human NCI-H661 cells incubated for 96 hrs by cell-titer Glo reagent based assay	[PMID: 26275028]
PC-9	IC₅₀	0.27 μM Compound: CO-1686	Anti-proliferative activity against human PC-9 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay Anti-proliferative activity against human PC-9 cells assessed as reduction in cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35594654]
PC-9	IC₅₀	211 nM Compound: CO-1686	Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysis Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells after 1 hr by Western blot analysis	[PMID: 26968253]
PC-9	GI₅₀	7 nM Compound: CO-1686	Antiproliferative activity against EGFR Del ex19 mutant expressing human PC9 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis Antiproliferative activity against EGFR Del ex19 mutant expressing human PC9 cells assessed as cell viability after 72 hrs by CellTiterGlo analysis	[PMID: 26968253]
PC-9	IC₅₀	79 nM Compound: 8; CO-1686	Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA	[PMID: 26756222]
Sf9	IC₅₀	0.002 μM Compound: CO-1686	Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of wild type EGFR (unknown origin) expressed in Sf9 cells pre-incubated for 30 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.002 μM Compound: CO-1686	Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	0.003 μM Compound: CO-1686	Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay Inhibition of EGFR L858R/T790M mutant (unknown origin) expressed in Sf9 cells pre-incubated for 60 mins before substrate and ATP addition by homogeneous time-resolved FRET assay	[PMID: 26275028]
Sf9	IC₅₀	21.5 nM Compound: 4	Inhibition of human recombinant N-terminal GST-tagged EGFR T790M/L858R double mutant cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay Inhibition of human recombinant N-terminal GST-tagged EGFR T790M/L858R double mutant cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay	[PMID: 27634676]
Sf9	IC₅₀	460 nM Compound: 4	Inhibition of human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay Inhibition of human recombinant N-terminal GST-tagged wild type EGFR cytoplasmic domain (695 end residues) autophosphorylation expressed in baculovirus infected Sf9 insect cells by ADP-Glo luminescence assay	[PMID: 27634676]
SW-620	IC₅₀	10.5 μM Compound: Rociletinib	Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]

体外研究
(In Vitro)

Rociletinib (CO-1686) (0.1 μM) 有效且不可逆地抑制 EGFR，并抑制 23 个靶标中超过 50% 的靶标。Rociletinib 有效且选择性地抑制表达突变型 EGFR 的 NSCLC 细胞的生长并诱导细胞凋亡。Rociletinib 耐药的 NSCLC 细胞系对 AKT 抑制敏感^[1]。

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

体内研究
(In Vivo)

Rociletinib (CO-1686) (100 mg/kg/天，口服) 在 NSCLC EGFR 突变体异种移植模型中表现出抗肿瘤活性。Rociletinib (CO-1686) (50 mg/kg bid，po) 在表达人 EGFR-L858R 和 EGFR-L858R-T790M 的转基因小鼠中表现出抗肿瘤活性^[1]。

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

Clinical Trial

分子量

555.55

Formula

C₂₇H₂₈F₃N₇O₃

CAS 号

1374640-70-6

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 125 mg/mL (225.00 mM; 超声助溶 (<60°C); 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	1.8000 mL	9.0001 mL	18.0002 mL
5 mM	0.3600 mL	1.8000 mL	3.6000 mL
10 mM	0.1800 mL	0.9000 mL	1.8000 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

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 (4.50 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.50 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。

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: 99.79%

选择批次：

Data Sheet (633 KB) SDS (393 KB)

COA (285 KB) LCMS (266 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25. [Content Brief]

Cell Assay ^[1]	Cells are seeded at 3,000 cells/well in growth media supplemented with 5% FBS, 2 mM L-glutamine, and 1 % P/S, allowed to adhere overnight, and treated with a dilution series of test compound (Rociletinib) for 72 hr. Cell viability is determined by CellTiter Glo and results are represented as background-subtracted relative light units normalized to a DMSO-treated control. Growth inhibition (GI₅₀) values are determined by GraphPad Prism 5.04. Combination index (CI) data is generated using CalcuSyn. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Briefly, NCr nu/nu mice are sub-cutaneously implanted with 1×10⁷ tumor cells in 50% Matrigel (injection volume of 0.2 mL/mouse). Once tumors reached 100-200 mm³, Animals are dosed with compounds (Rociletinib) as outlined (N=10 animals/gp). Briefly, LUM1686 PDX tumor fragments, harvested from donor mice, are inoculated into BALB/c nude mice. Administration of test compounds (Rociletinib (CO-1686)) is initiated at a mean tumor size of approximately 160 mm³. Tumor growth is monitored over time to determine tumor growth inhibition of the experimental agent vs. vehicle. The endpoint of the experiment is a mean tumor volume (MTV) in control group of 2000 mm³. Percent TGI is defined as the difference between the MTV of the designated control group and the MTV of the drug-treated group, expressed as a percentage of the MTV of the designated control group. Data is presented as mean±standard error of the mean (SEM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. Cancer Discov. 2013 Sep 25. [Content Brief]

Rociletinib 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	1.8000 mL	9.0001 mL	18.0002 mL	45.0005 mL
	5 mM	0.3600 mL	1.8000 mL	3.6000 mL	9.0001 mL
	10 mM	0.1800 mL	0.9000 mL	1.8000 mL	4.5000 mL
	15 mM	0.1200 mL	0.6000 mL	1.2000 mL	3.0000 mL
	20 mM	0.0900 mL	0.4500 mL	0.9000 mL	2.2500 mL
	25 mM	0.0720 mL	0.3600 mL	0.7200 mL	1.8000 mL
	30 mM	0.0600 mL	0.3000 mL	0.6000 mL	1.5000 mL
	40 mM	0.0450 mL	0.2250 mL	0.4500 mL	1.1250 mL
	50 mM	0.0360 mL	0.1800 mL	0.3600 mL	0.9000 mL
	60 mM	0.0300 mL	0.1500 mL	0.3000 mL	0.7500 mL
	80 mM	0.0225 mL	0.1125 mL	0.2250 mL	0.5625 mL
	100 mM	0.0180 mL	0.0900 mL	0.1800 mL	0.4500 mL

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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.

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Rociletinib (Synonyms: CO-1686; AVL-301; CNX-419)

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Rociletinib (Synonyms: CO-1686; AVL-301; CNX-419)

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Other Forms of Rociletinib:

Rociletinib 相关抗体

MCE 顾客使用本产品发表的 13 篇科研文献

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