Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).
产品描述 | Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM). |
靶点活性 | c-Met:513 nM (kd), RET:2 nM (kd), Lck:2 nM (kd), MEK1:7100 nM (kd), Abl-1:3 nM (kd), CSF1R:9 nM (kd), EphA2:14 nM (kd), MEK2:8300 nM (kd), VEGFR2:8 nM (kd), EGFR:22 nM (kd), Raf:39 nM (kd), JAK2:4700 nM (kd), c-Kit:2 nM (kd), B-Raf (V600E):14 nM (kd), BRAF:36 nM (kd) |
体外活性 | Agerafenib exhibits high potency against several BRAF V600E-dependent cell lines and selective cytotoxicity for tumor cell lines expressing mutant BRAF V600E. It shows potent binding (BRAF V600E, Kd: 14 nM) and cellular activity (pMEK IC50=82 nM and A375 proliferation IC50=78 nM), with activity in the proliferation assay. Agerafenib also exhibits a favorable CYP450 inhibition profile, with measured IC50 values greater than 10 μM versus the CYP1A2, CYP2C9, CYP2D6, and CYP3A4 isoforms and an IC50=3.4 μM versus CYP2C19. |
体内活性 | Agerafenib exhibits an exceptional PK profile in mouse, dog, and cynomolgus monkey. Administration of Agerafenib to beagle dogs (single dose of 1 mg/kg i.v and 10 mg/kg p.o) results in low clearance (CL=5.0 (mL/min)/kg) and excellent bioavailability (%F=100). Similarly, in cynomolgus monkey, the administration of Agerafenib (single dose of 1 mg/kg i.v and 10 mg/kg p.o) leads to high oral exposure due to low clearance (CL=6.7 mL/min/kg) and excellent bioavailability (%F=100). Oral administration of Agerafenib to Colo-205 tumor xenograft-bearing mice results in significant inhibition of pMEK in tumor cell lysates. |
别名 | RXDX-105 hydrochloride, CEP-32496 (hydrochloride) |
分子量 | 553.92 |
分子式 | C24H23ClF3N5O5 |
CAS No. | 1227678-26-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Agerafenib hydrochloride 1227678-26-3 Apoptosis Tyrosine Kinase/Adaptors c-RET c-Kit RXDX105 Hydrochloride CEP 32496 CEP-32496 RXDX-105 hydrochloride RXDX 105 Hydrochloride CEP32496 RXDX-105 Hydrochloride Agerafenib Hydrochloride CEP-32496 (hydrochloride) Inhibitor inhibitor inhibit