製品番号: HY-12047

Ponatinib

(別名: AP24534)

56 Cited Publications

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Based on 56 publication(s) in Google Scholar

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.

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純度: 99.67%
CAS 番号: 943319-70-8
分子式: C₂₉H₂₇F₃N₆O
分子量:532.56

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ponatinib 構造式

CAS 番号: 943319-70-8

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製品説明

IC₅₀ & Target^[1]

VEGFR2

1.5 nM (IC₅₀)

PDGFRα

1.1 nM (IC₅₀)

FGFR1

2.2 nM (IC₅₀)

c-Kit

12.5 nM (IC₅₀)

Bcr-Abl アイソフォーム固有の製品をすべて表示 :

Abl
Bcr-Abl

PDGFR アイソフォーム固有の製品をすべて表示 :

VEGFR アイソフォーム固有の製品をすべて表示 :

Src アイソフォーム固有の製品をすべて表示 :

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	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	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	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	1.2 nM Compound: Ponatinib, AP24534	Antiproliferative activity against mouse BA/F3 cells expressing wild type BCR-ABL Antiproliferative activity against mouse BA/F3 cells expressing wild type BCR-ABL	[PMID: 21561767]
BaF3	IC₅₀	1219 nM Compound: Ponatinib, AP24534	Antiproliferative activity against BCR-ABL-negative parental mouse BA/F3 cells Antiproliferative activity against BCR-ABL-negative parental mouse BA/F3 cells	[PMID: 21561767]
BaF3	IC₅₀	8.8 nM Compound: Ponatinib, AP24534	Antiproliferative activity against mouse BA/F3 cells expressing ABL T315I mutant Antiproliferative activity against mouse BA/F3 cells expressing ABL T315I mutant	[PMID: 21561767]
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	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	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	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	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	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	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	431.9 nM Compound: Ponatinib	Cytotoxicity against mouse BaF3 cells expressing IL-3 assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing IL-3 assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 28287083]
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	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	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	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]
HT-29	EC₅₀	50 nM Compound: Ponatinib	Anti-necroptosis activity against TNFalpha-induced human HT-29 cells assessed as reduction in cell viability Anti-necroptosis activity against TNFalpha-induced human HT-29 cells assessed as reduction in cell viability	[PMID: 38199165]
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	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]
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	EC₅₀	89 nM Compound: Ponatinib	Anti-necroptosis activity against TNFalpha-induced human Jurkat cells assessed as reduction in cell viability Anti-necroptosis activity against TNFalpha-induced human Jurkat cells assessed as reduction in cell viability	[PMID: 38199165]
K562	IC₅₀	0.023 μM Compound: AP24534, Ponatinib	Cytotoxicity against human K562 cells Cytotoxicity against human K562 cells	[PMID: 23600806]
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	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	IC₅₀	0.34 nM 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	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]
K562	IC₅₀	10 nM Compound: Ponatinib	Cytotoxicity against human K562 cells assessed as induction of cell death Cytotoxicity against human K562 cells assessed as induction of cell death	[PMID: 34011155]
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	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	GI₅₀	0.5 nM 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	EC₅₀	0.39 nM Compound: Ponatinib	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days in the presence of asciminib by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days in the presence of asciminib by celltiter-glo 2.0 assay	[PMID: 37849551]
K562	EC₅₀	0.4 nM Compound: Ponatinib	Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 3 days by celltiter-glo 2.0 assay	[PMID: 37849551]
K562	EC₅₀	1.49 nM Compound: Ponatinib	Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days in the presence of asciminib by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days in the presence of asciminib by celltiter-glo 2.0 assay	[PMID: 37849551]
K562	EC₅₀	1.77 nM Compound: Ponatinib	Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days by celltiter-glo 2.0 assay Antiproliferative activity against human K562 cells expressing ABL T315I mutant assessed as inhibition of cell growth incubated for 3 days by celltiter-glo 2.0 assay	[PMID: 37849551]
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]
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]
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]
L02	IC₅₀	64.7 μM Compound: Ponatinib	Cytotoxicity against human LO2 cells Cytotoxicity against human LO2 cells	[PMID: 31668972]
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	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]
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]
MV4-11	IC₅₀	0.3 nM Compound: 7	Inhibition of FLT3 in human MV4-11 cells Inhibition of FLT3 in human MV4-11 cells	10.1039/C1MD00175B
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	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]
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]
RPMI-8226	IC₅₀	124.7 nM Compound: Chemical probe : AP24534	Inhibition of BCR/ABL/FLT3/RET/KIT/FGFR/PDGFR in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Inhibition of BCR/ABL/FLT3/RET/KIT/FGFR/PDGFR in human RPMI-8226 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 26254279]
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-266	IC₅₀	720.6 nM Compound: Chemical probe : AP24534	Cytotoxicity against human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay Cytotoxicity against human U-266 cells assessed as reduction of cell growth incubated for 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay	[PMID: 26254279]
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]

体外実験

Ponatinib (AP24534) potently inhibits native ABL (IC₅₀: 0.37 nM), ABL^T315I (IC₅₀: 2.0 nM), and other clinically important ABL kinase domain mutants (IC₅₀: 0.30-0.44 nM). Ponatinib also inhibits SRC (IC₅₀: 5.4 nM) and members of the VEGFR, FGFR, and PDGFR families of receptor tyrosine kinases. Ponatinib potently inhibits proliferation of Ba/F3 cells expressing native BCR-ABL (IC₅₀: 0.5 nM). All BCR-ABL mutants tested remained sensitive to Ponatinib (IC₅₀: 0.5-36 nM) including BCR-ABL^T315I (IC₅₀: 11 nM)^[1].
Ponatinib inhibits the in vitro kinase activity of FLT3, KIT, FGFR1, and PDGFRα with IC₅₀ values of 13, 13, 2, and 1 nM, respectively. Ponatinib inhibits phosphorylation of all 4 RTKs in a dose-dependent manner, with IC₅₀ values between 0.3 to 20 nM. Consistent with these activated receptors being important in driving leukemogenesis Ponatinib also potently inhibits the viability of all 4 cell lines with IC₅₀ values of 0.5 to 17 nM. In contrast, the IC₅₀ for inhibition of RS4;11 cells which express native (unmutated) FLT3, is more than 100 nM^[2].

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

体内実験

In a survival model in which mice are instead injected with Ba/F3 BCR-ABL^T315I cells, administration of Dasatinib at doses as high as 300 mg/kg has no effect on survival time. By contrast, treatment with Ponatinib (AP24534) prolongs survival in a dose-dependent manner. Ponatinib dosed orally for 19 days at 5, 15, and 25 mg/kg prolongs median survival to 19.5, 26, and 30 days, respectively compare to 16 days for vehicle-treated mice (p<0.01 for all three dose levels). The anti-tumor activity of Ponatinib (AP24534) is further assessed in a xenograft model in which Ba/F3 BCR-ABL^T315I cells are injected subcutaneously into mice. Tumor growth is inhibited by Ponatinib in a dose-dependent manner compare to vehicle-treated mice, with significant suppression of tumor growth upon daily oral dosing at 10 and 30 mg/kg (%T/C = 68% and 20%, respectively; p<0.01 for both dose levels). Daily oral dosing of 50 mg/kg Ponatinib causes significant tumor regression (%T/C = 0.9%, p<0.01), with a 96% reduction in mean tumor volume at the final measurement compared to the start of treatment. Ponatinib is well tolerated at all efficacious dose levels for the duration of the study; maximal decreases in body weight are <5%, <5%, and <12% for the 10, 30, and 50 mg/kg dose groups, respectively, with no signs of overt toxicity^[1].
Ponatinib (1-25 mg/kg) is administered orally, once daily for 28 days, to mice bearing MV4-11 xenografts. Ponatinib potently inhibits tumor growth in a dose-dependent manner. Administration of 1 mg/kg, the lowest dose tested, leads to significant inhibition of tumor growth (TGI=46%, P<0.01) and doses of 2.5 mg/kg or greater results in tumor regression^[2].

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

化学情報

CAS 番号 943319-70-8
性状 Solid
分子量 532.56
分子式 C₂₉H₂₇F₃N₆O
Color Light yellow to yellow
SMILES

CC1=C(C=C(C=C1)C(NC2=CC(C(F)(F)F)=C(C=C2)CN3CCN(CC3)C)=O)C#CC4=CN=C5N4N=CC=C5
別名

AP24534
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (56)

All WBCell Imaging/StainingIn Vivo Efficacy StudyCell Proliferation/Viability Assay

Sort by:

Journal Impact Factor

Cancer Discov

TRK xDFG Mutations Trigger a Sensitivity Switch from Type I to II Kinase Inhibitors. [Abstract]

2021 Jan;11(1):126-141. PMID: 33004339
Nat Immunol

Sparcl1 mitigates abdominal aortic aneurysm through inhibiting lymphangiogenesis-mediated TLS formation. [Abstract]

2026 Apr;27(4):738-749. PMID: 41760906
Acta Pharm Sin B

A high-throughput Gaussia luciferase reporter assay for screening potential gasdermin E activators against pancreatic cancer. [Abstract]

2023 Oct;13(10):4253-4272. PMID: 37799380

Ponatinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Oct;13(10):4253-4272. [Abstract]

BxPC-3, PANC-1 and H6c7 cells were treated with ponatinib (0.1–20 μM) for 24 h, and then cell viability was analyzed by CCK-8 assay.

Ponatinib purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Oct;13(10):4253-4272. [Abstract]

PANC-1 cells were treated with Ponatinib (5-20 μM) or Perifosine (30-70 μM) for 24 h, and total cellular extracts were subjected to Western blot analyses using antibodies against GSDMD and β-tubulin.
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Adv Sci (Weinh)

BCR::ABL1-Induced Enhancer Reprogramming Uncovers Hypersensitivity of Ph+B-ALL Cells to Enhancer-Targeting Drugs. [Abstract]

2026 Mar 1:e17231. PMID: 41764406
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
MedComm (2020)

BCR-ABL1 Drives Transcriptional Reprogramming of Chronic Myeloid Leukemia Cells for Immune Evasion Through C/EBPβ. [Abstract]

2026 Apr 26:7:e70747. PMID: 42051376
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Int J Biol Macromol

Critical role of protein kinase CK2 in chronic myeloid leukemia cells harboring the T315I BCR::ABL1 mutation. [Abstract]

2024 Dec 2:138305. PMID: 39631575

Ponatinib purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2024 Dec 2:138305. [Abstract]

KBM5-T315I cells were treated with the indicated concentrations of CX-4945, Ponatinib (0.001-10 μM), or with two combined drugs by simultaneously increasing their concentration at the ratio of 1:500 for Ponatinib + CX-4945. Viability was assessed by the MTT method after 48 h treatment and expressed as percentage of vehicle-treated controls.
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Phytomedicine

Huang-Qi-Long-Dan Granule alleviates ischemic stroke injury by regulating the crosstalk between Nrf2 and NF-κB signaling. [Abstract]

2026 Jun:155:158069. PMID: 41861685
Biomed Pharmacother

Identification of nsp16 inhibitors of SARS -CoV-2, SARS -CoV-1 and MERS-CoV from FDA-approved drugs using in silico and in vitro methods. [Abstract]

2025 Jun 20:189:118246. PMID: 40543162
Biomed Pharmacother

Buparlisib and ponatinib inhibit aggressiveness of cholangiocarcinoma cells via suppression of IRS1-related pathway by targeting oxidative stress resistance. [Abstract]

2024 Nov:180:117569. PMID: 39418964

Ponatinib purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117569. [Abstract]

Ponatinib inhibited proliferation of CCA cell lines. Relative viability (%) of KKU-100 and KKU-213A cells after 48 h treatment with buparlisib, Ponatinib and the combination of both drugs (0.25-5 μM).

Ponatinib purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117569. [Abstract]

Intracellular ROS in KKU-100 and KKU-213A cells after exposure to 0.75 μM Buparlisib, 0.75 μM Ponatinib and the combination of both for 6 h was measured by fluorescence microscopy using DCFH-DA staining.

Ponatinib purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117569. [Abstract]

Representative image of tumors dissected from KKU-213A xenograft mice after 14 days of treatment with Buparlisib (15 mg/kg/day), Ponatinib (30 mg/kg/day) and their combination.
J Med Chem

A Fast Method to Monitor Tyrosine Kinase Inhibitor Mechanisms. [Abstract]

2024 Nov 28;67(22):20571-20579. PMID: 39513680
J Med Chem

Discovery of ( E)- N1-(3-Fluorophenyl)- N3-(3-(2-(pyridin-2-yl)vinyl)-1 H-indazol-6-yl)malonamide (CHMFL-KIT-033) as a Novel c-KIT T670I Mutant Selective Kinase Inhibitor for Gastrointestinal Stromal Tumors (GISTs). [Abstract]

2019 May 23;62(10):5006-5024. PMID: 31046271
Neurosci Bull

Role of Elevated Thrombospondin-1 in Kainic Acid-Induced Status Epilepticus. [Abstract]

2020 Mar;36(3):263-276. PMID: 31664678
Biochem Pharmacol

Inhibition of AKR1B10-mediated metabolism of daunorubicin as a novel off-target effect for the Bcr-Abl tyrosine kinase inhibitor dasatinib. [Abstract]

2021 Oct:192:114710. PMID: 34339712
J Ethnopharmacol

Reinwardtia indica Dumort. protects against ponatinib-induced cerebral ischemia in adult zebrafish via attenuation of oxidative stress, neuroinflammation, mitochondrial dysfunction, and neurotransmitter dysregulation: A multi-target therapeutic strategy. [Abstract]

2025 Sep 17;355(Pt A):120621. PMID: 40972727
J Ethnopharmacol

Alleviation of endothelial dysfunction of Pheretima guillemi (Michaelsen)-derived protein DPf3 in ponatinib-induced thrombotic zebrafish and mechanisms explored through ox-LDL-induced HUVECs and TMT-based proteomics. [Abstract]

2024 Apr 6:323:117669. PMID: 38159828
J Ethnopharmacol

Determining the chemical profile of Caragana jubata (Pall.) Poir. by UPLC-QTOF-MS analysis and evaluating its anti-ischemic stroke effects. [Abstract]

2023 Jun 12:309:116275. PMID: 36806344
Commun Biol

Glutathione determines chronic myeloid leukemia vulnerability to an inhibitor of CMPK and TMPK. [Abstract]

2024 Jul 10;7(1):843. PMID: 38987326
Int J Mol Sci

Inhibition of Fibroblast Growth Factor Receptor 3 Signaling by Ponatinib Reduces Growth and Cytokine Production of Multiple Myeloma Cells. [Abstract]

2026 Jun 9;27(12):5217. PMID: 42352940
Pharm Biol

The role of salvianolic acid B and benzoylpaeoniflorin in enhancing angiogenesis through Nrf2/HO-1/VEGFA signaling axis in ischemic stroke recovery. [Abstract]

2026 Dec;64(1):67-86. PMID: 41433220
Pharmaceuticals (Basel)

Discovering a Multi-Component Combination against Vascular Dementia from Danshen-Honghua Herbal Pair by Spectrum-Effect Relationship Analysis. [Abstract]

2022 Aug 29;15(9):1073. PMID: 36145294
Biomolecules

Investigating the Effect of Tyrosine Kinase Inhibitors on the Interaction between Human Serum Albumin by Atomic Force Microscopy. [Abstract]

2022 Jun 11;12(6):819. PMID: 35740944
Eur J Pharmacol

Ponatinib-induced ischemic stroke in larval zebrafish for drug screening. [Abstract]

2020 Dec 15;889:173292. PMID: 32668288
BMC Chem

Integrating analytical quality by design into bioanalytical method development: an HPLC-FLD method for quantification of alectinib in biological matrix. [Abstract]

2025 Aug 22;19(1):248. PMID: 40847406
Cancer Sci

CML With Mutant ASXL1 Showed Decreased Sensitivity to TKI Treatment via Upregulation of the ALOX5-BLTR Signaling Pathway. [Abstract]

2025 Apr;116(4):1115-1125. PMID: 39905783
Transl Oncol

A RIPK2 activity signature in prostate cancer: Modulation by RIPK2 inhibition and clinical association. [Abstract]

2026 Jul:69:102819. PMID: 42143470
J Inflamm Res

Qimai Feiluoping Decoction Inhibits EndMT to Alleviate Pulmonary Fibrosis by Reducing PI3K/AKT/mTOR Pathway-Mediated the Restoration of Autophagy. [Abstract]

2025 Jun 26:18:8447-8475. PMID: 40589610
J Hypertens

KAT7 contributes to ponatinib-induced hypertension by promoting endothelial senescence and inflammatory responses through activating NF-κB signaling pathway. [Abstract]

2025 May 1;43(5):827-840. PMID: 40084466
Target Oncol

In Vitro Comparison of the Effects of Imatinib and Ponatinib on Chronic Myeloid Leukemia Progenitor/Stem Cell Features. [Abstract]

2020 Oct;15(5):659-671. PMID: 32780298
Sci Rep

Functional personalized complex combination nano therapy for osteosarcoma. [Abstract]

2025 Oct 16;15(1):36227. PMID: 41102354
Sci Rep

Unraveling chain specific ubiquitination in cells using tandem ubiquitin binding entities. [Abstract]

2025 Jul 2;15(1):22961. PMID: 40595035
Heliyon

Quality by design-based approach for the development of an analytical method for quantifying ponatinib in rat plasma. [Abstract]

2024 Sep 28;10(19):e38637. PMID: 39403541
Clin Chim Acta

Investigation of metabolic stability of the novel ALK inhibitor brigatinib by liquid chromatography tandem mass spectrometry. [Abstract]

2018 May:480:180-185. PMID: 29458050
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
PLoS One

Chorioallantoic membrane (CAM) assay to study treatment effects in diffuse intrinsic pontine glioma. [Abstract]

2022 Feb 14;17(2):e0263822. PMID: 35157705
PLoS One

Analysis of acute lymphoblastic leukemia drug sensitivity by changes in impedance via stromal cell adherence. [Abstract]

2021 Sep 30;16(9):e0258140. PMID: 34591931
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Leuk Res

BCR/ABL increases EZH2 levels which regulates XIAP expression via miRNA-219 in chronic myeloid leukemia cells. [Abstract]

2016 Jun:45:24-32. PMID: 27070757
J Chem Eng Data

2024 Jun 10.
Exp Hematol

Hes1 upregulation contributes to the development of FIP1L1-PDGRA-positive leukemia in blast crisis. [Abstract]

2014 May;42(5):369-379.e3. PMID: 24486648

Ponatinib purchased from MedChemExpress. Usage Cited in: Exp Hematol. 2014 May;42(5):369-379.e3. [Abstract]

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 Ponatinib (0.1-1 μM) for 15 min. Data are representative of three independent experiments.
Biomed Rep

Toxicity evaluation and anti-ischemic stroke activity of selected natural extracts in zebrafish. [Abstract]

2026 Jun 24;25(2):99. PMID: 42388451
Pharmacogn Mag

2023 Jul 20.
Blood Neoplasia

From cell lines to PDXs: in vivo confirmation of synergistic drug responses identified in leukemia cell line models. [Abstract]

2026 Apr 9;3(3):100230. PMID: 42294111
chemRxiv

2026 Apr 6.
Blood Vessel Thromb Hemost

2025 Nov 17.
bioRxiv

2025 Sep 30.
bioRxiv

Identification of a RIPK2-Regulated Gene Signature as a Candidate Biomarker for RIPK2 Activity and Prognosis in Prostate Cancer. [Abstract]

2025 May 5:2025.04.30.651490. PMID: 40654646
University of Pittsburgh

2025.
bioRxiv

2025 February 26.
bioRxiv

SON-dependent nuclear speckle rehabilitation alleviates proteinopathies. [Abstract]

2025 Apr 28:2024.04.18.590103. PMID: 38659924
Research Square Print

2023 Mar 23.
Research Square Preprint

2021 May.
Technical University of Munich

24.01.2018.

溶剤 & 溶解度

体外:

DMSO : 25 mg/mL (46.94 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

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濃度 _(開始) 濃度 _(開始)

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濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

プロトコル

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].

MedChemExpress (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.

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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元素分析報告書 (2659 KB)
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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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

Ponatinib

56 Cited Publications

100 mg お問い合わせ

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Ponatinib

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MedChemExpress（MCE）の使用を引用している文献 Ponatinib

Bcr-Abl アイソフォーム固有の製品をすべて表示

PDGFR アイソフォーム固有の製品をすべて表示

VEGFR アイソフォーム固有の製品をすべて表示

Src アイソフォーム固有の製品をすべて表示

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化学情報

Publications (56)

溶剤 & 溶解度

プロトコル

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Ponatinib 関連分類

HY-12047 関連分類