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).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 18,500 | |||
5 mg | 在庫あり | ¥ 45,500 | |||
10 mg | 在庫あり | ¥ 67,500 | |||
25 mg | 在庫あり | ¥ 114,500 | |||
50 mg | 在庫あり | ¥ 160,000 | |||
100 mg | 在庫あり | ¥ 225,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 45,500 |
説明 | 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. |
分子量 | 382.78 |
分子式 | 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. 詳細
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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