Bcr-Abl

Inhibitory Selectivity

Catalog No.	Inhibitor Name	Bcr-Abl	Abl	Other
A10290	Dasatinib	****	****	Src,c-Kit (D816V),c-Kit (wt)
A10468	Imatinib Mesylate		*	c-Kit,PDGFR
A10108	Saracatinib		**	c-Src,LCK,EGFR (L861Q)
A10080	Ponatinib	****	****	PDGFRα,VEGFR2,FGFR1
A10644	Nilotinib	**
A10715	Danusertib	**	**	Aurora A,TrkA,RET
A10095	AT9283		***	JAK3,JAK2,Aurora B
A10988	Degrasyn	*		DUB
A10119	Bafetinib	***	***	Lyn
A10508	KW-2449	**	***	FLT3 (D835Y),FLT3,FGFR1
A10661	NVP-BHG712		*	EphB4,C-Raf,c-Src
A11200	Rebastinib		***	FLT3,KDR,Tie-2
A15849	GZD824 Dimesylate	****	****
A11439	GNF-2	*
A15887	GNF-7	***	*
A13029	Radotinib	**
A16320	Dasatinib Monohydrate	****	****	Src,c-Kit (D816V),c-Kit (wt)
A13237	GNF-5	*
A13120	PD173955	***		Src
A11379	DPH
A13530	Flumatinib mesylate		****	PDGFRβ, c-Kit

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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AP24534 (Ponatinib)

Catalog No. A10080
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BCR-ABL 抑制剂

AP24534 (Ponatinib)是有效的多激酶和pan-BCR-ABL抑制剂。了解更多

Product Citations (6)

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- Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Yamamoto Y, .et al. Development of a sandwich enzyme-linked immunosorbent assay for the quantification of ponatinib in serum, Anal Biochem, 2019, Feb 13. pii: S0003-2697(18)31083-2 PMID: 30771339
- N Naganna, .et al. Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice, EBioMedicine, 2019, Jan 24. pii: S2352-3964(19)30012-X PMID: 30686755
- Takuya Hirao, .et al. Altered intracellular signaling by imatinib increases the anti-cancer effects of tyrosine kinase inhibitors in chronic myelogenous leukemia cells, Cancer Sci, 2018, Jan; 109(1): 121-131 PMID: 29121435
- Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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NVP-BHG712

Catalog No. A10661
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EphB4 抑制剂

NVP-BHG712是EphB4激酶的选择性抑制剂，在体外对EphB4的选择性超过40多种其他激酶（包括FGFR3）。了解更多

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- Y Kaibori, .et al. EphA2 phosphorylation at Ser897 by the Cdk1/MEK/ERK/RSK pathway regulates M-phase progression via maintenance of cortical rigidity, the FASEB Journal, 2019, Jan 22:fj201801519RR PMID: 30668924
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Danusertib (PHA-739358)

Catalog No. A10715
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Aurora 抑制剂

Danusertib (PHA-739358)是Aurora A/B/C的Aurora激酶抑制剂，在无细胞分析中的IC50为13 nM/79nM/61 nM，对Abl，TrkA，c-RET和FGFR1以及更低的浓度具有中等效力对Lck，VEGFR2/3，c-Kit，CDK2等有效。了解更多

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- Samuel Q. Li, etc. Targeting Wild-Type and Mutationally Activated FGFR4 in Rhabdomyosarcoma with the Inhibitor Ponatinib (AP24534). PLoS One. 2013; 8(10): e76551.
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XL-228

Catalog No. A13069
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IGF-1R, Aurora, FGFR, ABL, SRC 抑制剂

XL228是靶向IGF1R，AURORA激酶，FGFR1-3，ABL和SRC家族激酶的蛋白激酶抑制剂。XL228是一种Aurora A抑制剂（IC50，f3 nmol/L），对ABL1（Ki，5 nmol/L）以及BCR-ABL1 T315I（Ki，1.4 nmol/L）激酶显示出有效的生化活性。了解更多

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KW-2449

Catalog No. A10508
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FLT3/FGFR/Bcr-Abl/Aurora 抑制剂

KW-2449是FLT3、ABl、ABl-T315I和Aurora激酶的多激酶抑制剂。了解更多

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