Ponatinib (Synonyms: 普纳替尼; AP24534)

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摩尔计算器

Ponatinib (AP24534) 是一种有效的，具有口服活性的多靶点激酶抑制剂，抑制 Abl，PDGFRα，VEGFR2，FGFR1 和 Src 的 IC₅₀ 分别为 0.37 nM， 1.1 nM，1.5 nM，2.2 nM 和 5.4 nM。

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Ponatinib Chemical Structure

CAS No. : 943319-70-8

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥593	In-stock
5 mg	￥506	In-stock
10 mg	￥810	In-stock
25 mg	￥1533	In-stock
50 mg	￥2300	In-stock
100 mg	￥3200	In-stock
200 mg	￥4925	In-stock
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Customer Review

Other Forms of Ponatinib:

MCE 顾客使用本产品发表的 31 篇科研文献

: Ponatinib purchased from MCE. Usage Cited in: Exp Hematol. 2014 May;42(5):369-379.e3. [Abstract]; (B,D) Phosphorylation levels of F/P (or its mutant), STAT5, or ERK in lysates of CMPs expressing Hes1 with F/P, F/P-D842V, or F/P-T674I, which have been treated with indicated doses of (B) Imatinib or (D) Ponatinib for 15 min. Data are representative of three independent experiments.

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PDGFR PDGFRβ PDGFRα

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Lck Fyn Blk

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC₅₀s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively^[1].

IC₅₀ & Target^[1]

VEGFR2

1.5 nM (IC₅₀)

PDGFRα

1.1 nM (IC₅₀)

FGFR1

2.2 nM (IC₅₀)

c-Kit

12.5 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	5.3 μM Compound: Ponatinib	Antiproliferative activity against human A549 cells expressing EGFR assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells expressing EGFR assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 31668972]
BaF3	IC₅₀	0.0023 μM Compound: AP24534, Ponatinib	Cytotoxicity against mouse BA/F3 cells transfected with wild type Bcr-Abl after 48 hrs by XTT assay Cytotoxicity against mouse BA/F3 cells transfected with wild type Bcr-Abl after 48 hrs by XTT assay	[PMID: 23600806]
BaF3	IC₅₀	0.006 μM Compound: 3, AP24534	Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay Antiproliferative activity against mouse BA/F3 cells expressing Bcr-Abl T315I mutant after 72 hrs by CCK-8 assay	[PMID: 26195136]
BaF3	IC₅₀	0.0073 μM Compound: Ponatinib	Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay Cytotoxicity against mouse BA/F3 cells expressing BCR-ABL T315I mutant after 72 hrs by MTT assay	[PMID: 26814890]
BaF3	EC₅₀	0.05 nM Compound: Ponatinib	Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Inhibition of human wild type BCR-ABL expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27010810]
BaF3	EC₅₀	0.3 nM Compound: Ponatinib	Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 27010810]
BaF3	IC₅₀	0.9 nM Compound: Ponatinib	Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against mouse BAF3 cells expressing native BCR-ABL assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
BaF3	IC₅₀	1.2 nM Compound: 20g, AP24534	Antiproliferative activity against mouse BA/F3 cells expressing wild type ABL after 3 days by MTS assay Antiproliferative activity against mouse BA/F3 cells expressing wild type ABL after 3 days by MTS assay	[PMID: 20513156]
BaF3	IC₅₀	1.9 μM Compound: AP24534, Ponatinib	Cytotoxicity against mouse BA/F3 cells after 48 hrs by XTT assay Cytotoxicity against mouse BA/F3 cells after 48 hrs by XTT assay	[PMID: 23600806]
BaF3	EC₅₀	10.6 nM Compound: Ponatinib	Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay Protac activity at Cereblon/BCR/ABL T315I mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in BCR-ABL T315I mutant driven cell viability incubated for 3 days by CCK8 assay	[PMID: 32657579]
BaF3	IC₅₀	1219 nM Compound: 20g, AP24534	Antiproliferative activity against mouse BA/F3 cells after 3 days by MTS assay Antiproliferative activity against mouse BA/F3 cells after 3 days by MTS assay	[PMID: 20513156]
BaF3	IC₅₀	126.8 nM Compound: Ponatinib	Antiproliferative activity against mouse BAF3 cells expressing TEL-FGFR4 fusion protein after 72 hrs by CCK8/SRB assay Antiproliferative activity against mouse BAF3 cells expressing TEL-FGFR4 fusion protein after 72 hrs by CCK8/SRB assay	[PMID: 27750146]
BaF3	IC₅₀	136 nM Compound: AP24534	Inhibition of CCDC6/RET V804M mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay Inhibition of CCDC6/RET V804M mutant (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay	[PMID: 27815117]
BaF3	IC₅₀	180.4 nM Compound: AP24534	Inhibition of CCDC6/RET (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay Inhibition of CCDC6/RET (unknown origin) expressed in mouse BaF3 cells assessed as reduction in cell proliferation after 72 hrs by MTT assay	[PMID: 27815117]
BaF3	IC₅₀	39.1 nM Compound: Ponatinib	Antiproliferative activity against mouse BAF3 cells expressing CCDC6-RET fusion protein after 72 hrs by CCK8/SRB assay Antiproliferative activity against mouse BAF3 cells expressing CCDC6-RET fusion protein after 72 hrs by CCK8/SRB assay	[PMID: 27750146]
BaF3	EC₅₀	438 nM Compound: Ponatinib	Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay Antiproliferative activity against wild type mouse BA/F3 cells incubated for 3 days by CCK8 assay	[PMID: 32657579]
BaF3	IC₅₀	53.7 nM Compound: Ponatinib	Antiproliferative activity against mouse BAF3 cells expressing TEL-KDR fusion protein after 72 hrs by CCK8/SRB assay Antiproliferative activity against mouse BAF3 cells expressing TEL-KDR fusion protein after 72 hrs by CCK8/SRB assay	[PMID: 27750146]
BaF3	IC₅₀	71.5 nM Compound: Ponatinib	Antiproliferative activity against mouse BAF3 cells expressing CCDC6-RET V840M mutant after 72 hrs by CCK8/SRB assay Antiproliferative activity against mouse BAF3 cells expressing CCDC6-RET V840M mutant after 72 hrs by CCK8/SRB assay	[PMID: 27750146]
BaF3	IC₅₀	8.8 nM Compound: 20g, AP24534	Antiproliferative activity against mouse BA/F3 cells expressing ABL T315I mutant after 3 days by MTS assay Antiproliferative activity against mouse BA/F3 cells expressing ABL T315I mutant after 3 days by MTS assay	[PMID: 20513156]
BaF3	IC₅₀	9.6 nM Compound: Ponatinib	Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay Cytotoxicity against mouse BAF3 cells expressing BCR-ABL T315I mutant assessed as inhibition of cell growth measured after 48 hrs by trypan blue assay	[PMID: 34011155]
BXPC-3	EC₅₀	544 nM Compound: Ponatinib	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 27010810]
CAKI-2	EC₅₀	653 nM Compound: Ponatinib	Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay	[PMID: 27010810]
GIST430	GI₅₀	149 nM Compound: 4	Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay	[PMID: 28991465]
GISTT1	GI₅₀	106 nM Compound: 4	Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay	[PMID: 28991465]
GISTT1	GI₅₀	17 nM Compound: 4	Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay	[PMID: 28991465]
GISTT1	GI₅₀	40 nM Compound: 4	Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay	[PMID: 28991465]
H9c2	EC₅₀	379 nM Compound: Ponatinib	Antiproliferative activity against rat H9C2 cells incubated for 3 days by CCK8 assay Antiproliferative activity against rat H9C2 cells incubated for 3 days by CCK8 assay	[PMID: 32657579]
HEK293	IC₅₀	1.12 μM Compound: AP24534	Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability measured after 48 hrs by alamar blue assay	[PMID: 35944901]
Hep 3B2	IC₅₀	0.72 μM Compound: 5	Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human Hep3B cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 37196426]
HepG2	IC₅₀	> 5 μM Compound: ponatinib	Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 25835317]
HepG2	IC₅₀	0.6 μM Compound: Ponatinib	Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells expressing VEGFR2 assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 31668972]
HT-29	EC₅₀	440 nM Compound: Ponatinib	Anti-necroptic activity in human HT-29 cells assessed as inhibition of TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis incubated for 24 hrs by celltiter-glo luminescent cell viability assay Anti-necroptic activity in human HT-29 cells assessed as inhibition of TSZ (TNFalpha, Smac mimetic and z-VAD-FMK) induced necroptosis incubated for 24 hrs by celltiter-glo luminescent cell viability assay	[PMID: 36136378]
Huh-7	IC₅₀	0.99 μM Compound: 5	Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay Antiproliferative activity against human Huh-7 cells assessed as inhibition of cell growth measured after 72 hrs by CCK8 assay	[PMID: 37196426]
HUVEC	IC₅₀	0.5 μM Compound: Ponatinib	Antiproliferative activity against human HUVEC cells expressing VEGFR2 assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human HUVEC cells expressing VEGFR2 assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 31668972]
HUVEC	EC₅₀	515 nM Compound: Ponatinib	Antiproliferative activity against human HUVEC incubated for 3 days by CCK8 assay Antiproliferative activity against human HUVEC incubated for 3 days by CCK8 assay	[PMID: 32657579]
Jurkat	IC₅₀	295 nM Compound: Ponatinib	Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human Jurkat cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
Jurkat	IC₅₀	34 nM Compound: 6	Anti-necroptic activity in TNF alpha stimulated FADD-deficient human Jurkat T cells incubated for 24 hrs by celltiter-glo luminescent cell viability assay Anti-necroptic activity in TNF alpha stimulated FADD-deficient human Jurkat T cells incubated for 24 hrs by celltiter-glo luminescent cell viability assay	[PMID: 36346971]
Jurkat	IC₅₀	34 nM Compound: 37	Anti-neprotic activity in human Jurkat cells assessed as reduction in TNF-induced necroptosis incubated for 24 hrs by cell titer glo-based luminescence assay Anti-neprotic activity in human Jurkat cells assessed as reduction in TNF-induced necroptosis incubated for 24 hrs by cell titer glo-based luminescence assay	[PMID: 31622096]
K562	IC₅₀	0.00034 μM Compound: Ponatinib	Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 26814890]
K562	GI₅₀	0.0005 μM Compound: AP24534	Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay Growth inhibition of human K562 cells measured after 48 hrs by alamarblue assay	[PMID: 35944901]
K562	IC₅₀	0.003 μM Compound: 3, AP24534	Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells expressing wild type Bcr-Abl after 72 hrs by CCK-8 assay	[PMID: 26195136]
K562	GI₅₀	0.004 μM Compound: AP24534	Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay Growth inhibition of human K562 cells expressing BCR-ABL T315I mutant measured after 48 hrs by alamarblue assay	[PMID: 35944901]
K562	IC₅₀	0.3 nM Compound: Ponatinib	Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay Antiproliferative activity against human K562 cells incubated for 3 days by CCK8 assay	[PMID: 32657579]
K562	IC₅₀	0.3 nM Compound: Ponatinib	Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34011155]
K-562R	IC₅₀	0.08 μM Compound: Ponatinib	Antiproliferative activity against human K-562R cells expressing Bcr-Abl T315I mutant assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human K-562R cells expressing Bcr-Abl T315I mutant assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 35561654]
K-562R	IC₅₀	0.093 μM Compound: Ponatinib	Antiproliferative activity against T315I mutant expressing human K-562R cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against T315I mutant expressing human K-562R cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 34547714]
KBM5	IC₅₀	10.2 nM Compound: PN	Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against Imatinib mesylate sensitive wild-type human KBM5 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
KBM5	IC₅₀	10.6 nM Compound: PN	Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against imatinib mesylate resistant wild-type human KBM5 cells expressing T315I mutant assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
KG-1	IC₅₀	17.2 nM Compound: Ponatinib	Antiproliferative activity against FGFR1-translocated human KG1 cells after 72 hrs by CCK8/SRB assay Antiproliferative activity against FGFR1-translocated human KG1 cells after 72 hrs by CCK8/SRB assay	[PMID: 27750146]
KU812 cell line	IC₅₀	0.1 nM Compound: Ponatinib	Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human KU812 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]
KU812 cell line	IC₅₀	8.5 nM Compound: PN	Cytotoxicity against Bcr-Abl expressing human KU812 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against Bcr-Abl expressing human KU812 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 34052717]
MDA-MB-231	IC₅₀	0.156 μM Compound: ponatinib	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 25835317]
MDA-MB-231	IC₅₀	10.5 μM Compound: Ponatinib	Antiproliferative activity against human MDA-MB-231 cells expressing EGFR assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells expressing EGFR assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 31668972]
MDA-MB-231	EC₅₀	483 nM Compound: Ponatinib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27010810]
NCI-H1581	IC₅₀	194.2 nM Compound: Ponatinib	Antiproliferative activity against FGFR2-amplified human NCI-H1581 cells after 72 hrs by CCK8/SRB assay Antiproliferative activity against FGFR2-amplified human NCI-H1581 cells after 72 hrs by CCK8/SRB assay	[PMID: 27750146]
NCI-H1975	EC₅₀	> 1000 nM Compound: Ponatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 27010810]
PC-3	EC₅₀	> 1000 nM Compound: Ponatinib	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 27010810]
RBL-2H3	IC₅₀	148.3 nM Compound: Ponatinib	Antiallergic activity against anti-DNP-IgE sensitized rat RBL-2H3 cells assessed as induction of degranulation by measuring beta-hexosaminidase release using P-nitrophenyl-N-acetyl-D-glucosamide as substrate measured after 1 hr by microplate reader Antiallergic activity against anti-DNP-IgE sensitized rat RBL-2H3 cells assessed as induction of degranulation by measuring beta-hexosaminidase release using P-nitrophenyl-N-acetyl-D-glucosamide as substrate measured after 1 hr by microplate reader	[PMID: 34476950]
RBL-2H3	CC₅₀	410 nM Compound: Ponatinib	Cytotoxicity against rat RBL2H3 cells assessed as cell viability incubated for 24 hrs by CCK-8 assay Cytotoxicity against rat RBL2H3 cells assessed as cell viability incubated for 24 hrs by CCK-8 assay	[PMID: 34476950]
RT-112	IC₅₀	736.5 nM Compound: Ponatinib	Antiproliferative activity against FGFR3-amplified human RT112 cells after 72 hrs by CCK8/SRB assay Antiproliferative activity against FGFR3-amplified human RT112 cells after 72 hrs by CCK8/SRB assay	[PMID: 27750146]
Sf9	IC₅₀	1.6 nM Compound: 37	Inhibition of recombinant GST-tagged RIPK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 4 hrs by ADP-Glo assay Inhibition of recombinant GST-tagged RIPK3 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 4 hrs by ADP-Glo assay	[PMID: 31622096]
Sf9	IC₅₀	12 nM Compound: 37	Inhibition of recombinant GST-tagged RIPK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 4 hrs by ADP-Glo assay Inhibition of recombinant GST-tagged RIPK1 (unknown origin) expressed in baculovirus infected Sf9 insect cells incubated for 4 hrs by ADP-Glo assay	[PMID: 31622096]
SNU-16	IC₅₀	33.6 nM Compound: Ponatinib	Antiproliferative activity against FGFR2-amplified human SNU16 cells after 72 hrs by CCK8/SRB assay Antiproliferative activity against FGFR2-amplified human SNU16 cells after 72 hrs by CCK8/SRB assay	[PMID: 27750146]
U-937	IC₅₀	245.8 nM Compound: Ponatinib	Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Cytotoxicity against human U-937 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 34011155]

体外研究
(In Vitro)

Ponatinib (AP24534) 有效抑制天然 ABL (IC₅₀：0.37 nM)、ABL^T315I (IC₅₀：2.0 nM) 和其他临床重要的 ABL 激酶结构域突变体 (IC₅₀：0.30-0.44 nM)。Ponatinib 还抑制 SRC (IC₅₀：5.4 nM) 和受体酪氨酸激酶的 VEGFR、FGFR 和 PDGFR 家族成员。Ponatinib 有效抑制表达天然 BCR-ABL 的 Ba/F3 细胞的增殖 (IC₅₀：0.5 nM)。测试的所有 BCR-ABL 突变体对 Ponatinib (IC₅₀：0.5-36 nM) 保持敏感，包括 BCR-ABL^T315I (IC₅₀：11 nM)^[1]。
Ponatinib 抑制 FLT3、KIT、FGFR1 和 PDGFRα 的体外激酶活性，IC₅₀ 值分别为 13、13、2 和 1 nM。Ponatinib 以剂量依赖性方式抑制所有 4 种 RTK 的磷酸化，IC₅₀ 值在 0.3 到 20 nM 之间。与这些激活的受体在驱动白血病发生中起重要作用一致，Ponatinib 还有效抑制所有 4 种细胞系的活力，IC₅₀ 值为 0.5 至 17 nM。相比之下，抑制表达天然 (未突变) FLT3 的 RS4；11 细胞的 IC₅₀ 超过 100 nM^[2]。

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

体内研究
(In Vivo)

在小鼠改为注射 Ba/F3 BCR-ABL^T315I 细胞的生存模型中，以高达 300 mg/kg 的剂量施用达沙替尼对生存时间没有影响。相比之下，Ponatinib (AP24534) 处理以剂量依赖的方式延长了生存期。Ponatinib 以 5、15 和 25 mg/kg 的剂量口服给药 19 天，分别将中位生存期延长至 19.5、26 和 30 天，而载体处理的小鼠为 16 天 (所有三个剂量水平的 p <0.01)。Ponatinib (AP24534) 的抗肿瘤活性在异种移植模型中得到进一步评估，在该模型中，Ba/F3 BCR-ABL^T315I 细胞被皮下注射到小鼠体内。与媒介物处理的小鼠相比，Ponatinib 以剂量依赖性方式抑制肿瘤生长，每日口服给药 10 和 30 mg/kg 时肿瘤生长显著抑制 (%T/C 分别=68% 和 20%；对于两个剂量水平，p<0.01)。每日口服剂量为 50 mg/kg 的 Ponatinib 会导致显著的肿瘤消退 (%T/C=0.9%，p<0.01)，与处理开始时相比，最终测量的平均肿瘤体积减少 96%。在研究期间，Ponatinib 在所有有效剂量水平下均具有良好的耐受性；10、30 和 50 mg/kg 剂量组的体重最大下降分别为 <5%、<5% 和 <12%，没有明显的毒性迹象^[1]。
Ponatinib (1-25 mg/kg) 口服给药，每天一次，持续 28 天，给携带 MV4-11 异种移植物的小鼠。Ponatinib 以剂量依赖性方式有效抑制肿瘤生长。给予 1 mg/kg (最低测试剂量) 可显著抑制肿瘤生长 (TGI=46%，P<0.01)，2.5 mg/kg 或更高剂量可导致肿瘤消退^[2]。

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

Clinical Trial

分子量

532.56

Formula

C₂₉H₂₇F₃N₆O

CAS 号

943319-70-8

性状

固体

颜色

Light yellow to yellow

中文名称

帕纳替尼；帕拉替尼；泊那替尼；普纳替尼

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 : 25 mg/mL (46.94 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	1.8777 mL	9.3886 mL	18.7772 mL
5 mM	0.3755 mL	1.8777 mL	3.7554 mL
10 mM	0.1878 mL	0.9389 mL	1.8777 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 (4.69 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 (4.69 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 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。

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: 99.67%

选择批次：

Data Sheet (667 KB) SDS (420 KB)

COA (290 KB) HNMR (139 KB) LCMS (91 KB) 元素分析报告 (213 KB)

产品使用指南 (1538 KB)

参考文献

[1]. O'Hare T, et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell, 2009, 16(5), 401-412. [Content Brief]

[2]. Gozgit JM, et al. Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol Cancer Ther, 2011, 10(6), 1028-1035. [Content Brief]

[3]. Uchida T, et al. Hes1 upregulation contributes to the development of FIP1L1-PDGRA-positive leukemia in blast crisis. Exp Hematol. 2014 May;42(5):369-379.e3. [Content Brief]

Cell Assay ^[1]	Ba/F3 cell lines are distributed in 96-well plates (4×10³ cells/well) and incubated with escalating concentrations of Ponatinib for 72 hr. The inhibitor ranges used are: 0-625 nM for cells expressing BCR-ABL and 0-10,000 nM for BCR-ABL negative cells. Proliferation is measured using a methanethiosulfonate (MTS)-based viability assay. IC₅₀ values are reported as the mean of three independent experiments performed in quadruplicate. For cell proliferation experiments with CML or normal primary cells, mononuclear cells are plated in 96-well plates (5×10⁴ cells/well) over graded concentrations of Ponatinib (0-1000 nM) in RPMI supplemented with 10% FBS, L-glutamine, penicillin/streptomycin, and 100 μM β-mercaptoethanol. Following a 72 hr incubation, cell viability is assessed by subjecting cells to an MTS assay^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice^[1] For Ba/F3 survival model, Ba/F3 cells expressing native BCR-ABL or BCR-ABL^T315I are injected into the tail vein of female SCID mice (100 μL of a 1×10⁷ cells/mL suspension in serum-free medium). Beginning 72 hr later mice are treated once daily by oral gavage with vehicle (25 mM citrate buffer, pH 2.75), Ponatinib, or Dasatinib for up to 19 consecutive days. Moribund animals are sacrificed as per IACUC guidelines. On necropsy, mice have marked splenomegaly due to tumor cell infiltration. Survival data are analyzed using Kaplan-Meier method, and statistical significance is evaluated with a Log-rank test comparing the survival time of each treatment group with the vehicle group. For Ba/F3 Tumor Model, Ba/F3 BCR-ABL^T315I cells are implanted subcutaneously into the right flank of female nude mice (100 μL of a 1×10⁷ cells/mL cell suspension in serum-free medium). Mice are randomized to treatment groups when the average tumor volume reaches approximately 500 mm³. Mice are treated once daily by oral gavage with vehicle (25 mM citrate buffer, pH 2.75) or Ponatinib for up to 19 consecutive days. Tumor volume (mm³) is calculated. To determine tumor growth inhibition when the treatment period is finished, mean tumor volume for treatment group/mean tumor volume for control group (%T/C) is calculated at the final measurement. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. O'Hare T, et al. AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell, 2009, 16(5), 401-412. [Content Brief] [2]. Gozgit JM, et al. Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies. Mol Cancer Ther, 2011, 10(6), 1028-1035. [Content Brief] [3]. Uchida T, et al. Hes1 upregulation contributes to the development of FIP1L1-PDGRA-positive leukemia in blast crisis. Exp Hematol. 2014 May;42(5):369-379.e3. [Content Brief]

Ponatinib 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	1.8777 mL	9.3886 mL	18.7772 mL	46.9431 mL
	5 mM	0.3755 mL	1.8777 mL	3.7554 mL	9.3886 mL
	10 mM	0.1878 mL	0.9389 mL	1.8777 mL	4.6943 mL
	15 mM	0.1252 mL	0.6259 mL	1.2518 mL	3.1295 mL
	20 mM	0.0939 mL	0.4694 mL	0.9389 mL	2.3472 mL
	25 mM	0.0751 mL	0.3755 mL	0.7511 mL	1.8777 mL
	30 mM	0.0626 mL	0.3130 mL	0.6259 mL	1.5648 mL
	40 mM	0.0469 mL	0.2347 mL	0.4694 mL	1.1736 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.

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Ponatinib (Synonyms: 普纳替尼; AP24534)

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Ponatinib (Synonyms: 普纳替尼; AP24534)

Customer Review

Other Forms of Ponatinib:

Ponatinib 相关抗体

MCE 顾客使用本产品发表的 31 篇科研文献

Ponatinib 相关产品

•相关化合物库:

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查看 PDGFR 亚型特异性产品:

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Ponatinib 相关抗体:

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