Dabogratinib (TYRA-300) | FGFR3 inhibitor | Probechem Biochemicals

Chemical Structure : TYRA-300

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TYRA-300 (Dabogratinib, TYRA300)

货号: PC-23839Not For Human Use, Lab Use Only.

Dabogratinib (TYRA-300) is a potent, selective and oral FGFR3 inhibitor with IC50 of 11 nM in in Ba/F3 cells, 14-fold seletive over FGFR2 and >20-fold over FGFR1, FGFR4.

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生物&药学活性

Dabogratinib (TYRA-300) is a potent, selective and oral FGFR3 inhibitor with IC50 of 11 nM in in Ba/F3 cells, 14-fold seletive over FGFR2 and >20-fold over FGFR1, FGFR4.
TYRA-300 has 3-fold weaker against FGFR3 N540 K (IC50 = 73 nM).
TYRA-300 binds in the ATP pocket of FGFR3 through an extensive number of interactions.
TYRA-300 shows comparable potency in human bladder cancer cell lines harboring FGFR3 activating fusions or mutations.
TYRA-300 shows excellent kinome selectivity against a panel of 468 WT human kinases and mutant kinases.
TYRA-300 demonstrates equivalent potency for FGFR3 WT and V555M/L gatekeeper mutations in enzymatic assays and in engineered RT112/84 and UM-UC-14 bladder cancer cell lines containing the V555M mutation.
TYRA-300 at a dose of 12.5 mg/kg twice daily (BID) for 21 days produced significant inhibition of tumor growth (TGI) in T112/84 xenograft model (95% TGI).

物理化学性质&存储条件

分子量	559.47
分子式	C25H24Cl2N6O3S
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	5-[(1R)-1-(3,5-Dichloro-4-pyridyl)ethoxy]-3-[6-(2-methylsulfonyl-2,6-diazaspiro[3.3]heptan-6-yl)-3-pyridyl]-1H-indazole

参考文献

1. Hudkins RL, et al. J Med Chem. 2024 Sep 26;67(18):16737-16756.

TYRA-300 (Dabogratinib, TYRA300)

生物&药学活性

物理化学性质&存储条件

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TYRA-300 (Dabogratinib, TYRA300)

生物&药学活性

物理化学性质&存储条件

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