|6-(4-(3-氯-4-氟苯基)-1-(2-羟基乙基)-1H-咪唑-5-基)咪唑并[1,2-b]哒嗪-3-甲腈|CsnPharm

CAS No.: 2001559-19-7

BMS-986260 is a potent, selective, and orally bioavailable TGFβR1 inhibitor, with IC50 of 1.6 nM.

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400-920-2911

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描述TGFβ (transforming growth factor β) is a multifunctional cytokine that regulates a wide variety of biological processes that include cell proliferation, differentiation, migration and adhesion, and extracellular matrix modification including tumor stroma and immunosuppression. BMS-986260 is a selective and orally bioavailable TGFβR1 inhibitor with an IC₅₀ of 1.6 nM. BMS-986260 inhibited TGF-β mediated induction of regulatory T cell by downregulation of FOXP3 expression and a repression of CD25 with an IC₅₀ of 230 nM. In the MC38 murine colon carcinoma syngeneic model, combination of BMS-986260 with anti-PD-1-antibody demonstrated robust antitumor efficacy with a 90–100% complete response (CRs) at all 3 dose levels (3.75, 7.5, and 15 mg/kg). Additionally, BMS-986260 inhibited metastasis to the lungs in a 4T1 syngeneic orthotopic mammary tumor model^[1].
作用机制The hydroxyethyl group on the imidazole forms a hydrogen bond with Lys337^[1].
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