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BMS986260

CAT: 0013-GTR19156794-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19156794-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
BMS-986260 is a selective, and orally bioavailable TGFβR1 inhibitor (IC50 = 1.6 nM) . 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.
CAS Number
2001559-19-7
Purity
>98% (HPLC)
Solubility
In Vitro: DMSO : 125 mg/mL (326.56 mM)
Smiles
OCCn1cnc (c1-c1ccc2ncc (C#N) n2n1) -c1ccc (F) c (Cl) c1
Molecular Formula
C18H12ClFN6O
Molecular Weight
382.07
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.

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