Chemical Structure : TYRA-300
CAS No.:
2800223-30-5
TYRA-300
(TYRA300)
Catalog No.: PC-23839Not For Human Use, Lab Use Only.
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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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).
Physicochemical Properties
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M.Wt
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559.47
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Formula
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C25H24Cl2N6O3S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Hudkins RL, et al. J Med Chem. 2024 Sep 26;67(18):16737-16756.
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