Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 80.00 | |
5 mg | In stock | $ 198.00 | |
10 mg | In stock | $ 293.00 | |
25 mg | In stock | $ 498.00 | |
50 mg | In stock | $ 696.00 | |
100 mg | In stock | $ 983.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 198.00 |
Description | BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor(IC50 = 1.6 nM). |
In vitro | BMS-986260 demonstrated functional activity in multiple TGFβ-dependent cellular assays, excellent kinome selectivity, favorable pharmacokinetic properties, and curative in vivo efficacy in combination with anti-PD-1 antibody in murine colorectal cancer (CRC) models. Since daily dosing of TGFβR1 inhibitors is known to cause class-based cardiovascular (CV) toxicities in preclinical species, a dosing holiday schedule in the anti-PD-1 combination efficacy studies was explored. An intermittent dosing regimen of 3 days on and 4 days off allowed mitigation of CV toxicities in one month dog and rat toxicology studies and also provided similar efficacy as once daily dosing. |
Molecular Weight | 382.78 |
Formula | C18H12ClFN6O |
CAS No. | 2001559-19-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (65.31 mM)
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
BMS986260 2001559-19-7 Stem Cells TGF-beta/Smad nuclear translocation TGFβR1 FOXP3 expression MINK Transforming growth factor beta receptors BMS-986260 oral NHLF cells inhibit Inhibitor CD25 TGF-β Receptor pSMAD2/3 selective BMS 986260 inhibitor