Resigratinib (KIN-3248) | FGFR inhibitor | Probechem Biochemicals

Chemical Structure : KIN-3248

CAS No.: 2750709-91-0

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KIN-3248 (Resigratinib, KIN3248)

货号: PC-21321Not For Human Use, Lab Use Only.

Resigratinib (KIN-3248) is a next-generation, irreversible, orally available, small molecule pan-FGFR inhibitor with IC50 of 3.9/5.3/9.7 nM for FGFR1/2/3, potently inhibits FGFR2 and FGFR3 gatekeeper, molecular brake, and activation loop mutations with IC50 of 5-20 nM.

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5 mg	￥1880	In stock
10 mg	￥2880	In stock
25 mg	￥4880	In stock
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100 mg		Get quote

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生物&药学活性

Resigratinib (KIN-3248) is a next-generation, irreversible, orally available, small molecule pan-FGFR inhibitor with IC50 of 3.9/5.3/9.7 nM for FGFR1/2/3, potently inhibits FGFR2 and FGFR3 gatekeeper, molecular brake, and activation loop mutations with IC50 of 5-20 nM.
Resigratinib (KIN-3248) exhibits low nanomolar biochemical potency against wild-type FGFR family members as well as mutants associated with resistance to FGFR inhibitors (IC50 3.9-24.1 nM).
Resigratinib (KIN-3248) is active in human FGFR2-PHGDH fusion-positive CCLP-1 and FGFR2-OPTN fusion-positive ICC13-7 cholangiocarcinoma cell lines engineered to express wild-type or clinically relevant gatekeeper, molecular brake, and activation loop mutant alleles (EC50=2.4-9.9 nM).
Resigratinib (KIN-3248) induces dose-dependent tumor growth inhibition and regressions in FGFR inhibitor-resistant, patient-derived gastric cancer and cholangiocarcinoma models harboring secondary FGFR2 kinase domain mutations.
Resigratinib (KIN-3248) is highly-selective, potent and broad-spectrum activity against mutations in both the FGFR2 and FGFR3 kinase domains- including gatekeeper, molecular brake, and activation loop alterations.

物理化学性质&存储条件

分子量	523.54
分子式	C26H27F2N7O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	3-[2-(1-Cyclopropyl-4,6-difluoro-1H-benzimidazol-5-yl)ethynyl]-1-[(3S,5R)-5-(methoxymethyl)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl]-5-(methylamino)-1H-pyrazole-4-carboxamide

参考文献

1. Aleksandra Franovic, et al. 2022 ASCO Gastrointestinal Cancers Symposium.

KIN-3248 (Resigratinib, KIN3248)

生物&药学活性

物理化学性质&存储条件

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KIN-3248 (Resigratinib, KIN3248)

生物&药学活性

物理化学性质&存储条件

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