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BMS-986260

规格或纯度: 98%

CAS编号: 2001559-19-7
分子式: C₁₈H₁₂ClFN₆O
分子量: 382.8
PubChem编号: 122510453

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货号 (SKU)	包装规格	是否现货	价格	数量
B412813-1mg	1mg	现货
B412813-5mg	5mg	现货
B412813-10mg	10mg	现货
B412813-25mg	25mg	现货
B412813-50mg	50mg	现货
B412813-100mg	100mg	现货

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activin A receptor type 1 Inhibitor activin A receptor type 1B Inhibitor transforming growth factor beta receptor 1 Inhibitor

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基本描述

规格或纯度	98%
英文名称	BMS-986260
生化机理	BMS-986260 is a potent, selective, and orally bioavailable inhibitor of TGFβR1 with IC50 of 1.6 nM.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Information BMS-986260 is a potent, selective, and orally bioavailable inhibitor of TGFβR1 with IC50 of 1.6 nM.

名称和标识符

IUPAC Name	6-[5-(3-chloro-4-fluorophenyl)-3-(2-hydroxyethyl)imidazol-4-yl]imidazo[1,2-b]pyridazine-3-carbonitrile
INCHI	InChI=1S/C18H12ClFN6O/c19-13-7-11(1-2-14(13)20)17-18(25(5-6-27)10-23-17)15-3-4-16-22-9-12(8-21)26(16)24-15/h1-4,7,9-10,27H,5-6H2
InChi Key	VZZBCNXVZFAIQX-UHFFFAOYSA-N
Canonical SMILES	C1=CC(=C(C=C1C2=C(N(C=N2)CCO)C3=NN4C(=NC=C4C#N)C=C3)Cl)F
关联CAS	2001559-19-7
PubChem CID	122510453
分子量	382.8

关联配体

Ligand ID	10662
名称	BMS-986260
别名	BMS986260
类别	Synthetic organic
学名	6-[5-(3-chloro-4-fluorophenyl)-3-(2-hydroxyethyl)imidazol-4-yl]imidazo[1,2-b]pyridazine-3-carbonitrile
生物活性评价	BMS-986260 potently inhibits human and mouse TGFβR1 in biochemical assays, and it is highly selective for TGFβR1 over TGFβR2 . It modulates target-mediated responses in multiple TGFβ-dependent cellular assays, and produces therapeutic efficacy in combination with anti-PD-1 antibody in murine colorectal cancer (CRC) models. Cardiovascular (CV) toxicities from TGFβR1 inhibition were alleviated in preclinical models, using an intermittent dosing regimen (3 days on and 4 days off). This regimen did not diminish the efficacy achieved with once daily dosing. Potential off-targets (IC₅₀ values <1 μM in a HTRF kinome screen) that are not included in the interactions table include TNIK, MINK (MINK1), HGK (MAP4K4), CK1δ (CSNK1D), CK1ε (CSNK1E), and KDR (VEGFR2).
评价	BMS-986260 is a potent, selective and orally bioavailable TGFβR1 inhibitor, that was developed for immuno-oncology potential . The chemical structure of BMS-986260 is one of those claimed in patent WO2016140884A1 (Rigel Pharmaceuticals/Bristol-Myers Squibb). The PubChem CID match was obtained using the SMILES for BMS-986260 that was generated from the structure image presented in .

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参考文献

1. Velaparthi U, Darne CP, Warrier J, Liu P, Rahaman H, Augustine-Rauch K, Parrish K, Yang Z, Swanson J, Brown J et al.. (2020) Discovery of BMS-986260, a Potent, Selective, and Orally Bioavailable TGFβR1 Inhibitor as an Immuno-oncology Agent.. ACS Med Chem Lett, 11 (2): (172-178). [PMID:32071685]

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