| Bioactivity | ML786 is a potent and orally bioavailable Raf inhibitor, with IC50s of 2.1, 4.2, and 2.5 nM for V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC50=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 can be used for the research of cancers[1]. |
| Invitro | ML786 (3 小时) 抑制 A375 细胞中细胞外信号调节激酶 (ERK) (pERK) 的激酶磷酸化，IC50 为 60 nM[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> ML786 相关抗体: |
| In Vivo | ML786 (75 mg/kg；口服，每日一次，共 21 天) 可抑制免疫功能低下小鼠的皮下 A375 M 异种移植[1]。ML786 (75 mg/kg；单次口服) 可强烈抑制小鼠的 Raf 通路[1]。ML786 (10 mg/kg；口服) 在大鼠中的口服生物利用度为 85%，AUC1-24h 为 35.9 μM·h[1]。ML786 (1 mg/kg；静脉注射) 在大鼠中的血浆清除率为 0.44 L/h/kg，Vss 为 3.93 L/kg[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| CAS | 1237586-97-8 |
| Formula | C29H29F3N4O3 |
| Molar Mass | 538.56 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Gould AE, et, al. Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. J Med Chem. 2011 Mar 24;54(6):1836-46. |