Agerafenib hydrochloride
作者：齐岳
发布时间：2023-09-07
09:26:08
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产品名称：Agerafenib hydrochloride
产品描述：
| 产品描述 | Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM). |
| 靶点活性 | BRAF:36 nM （kd）, BRafV600E:14 nM （kd）, c-Kit:2 nM （kd）, JAK-2:4700 nM （kd）, CRAF:39 nM （kd）, EGFR:22 nM （kd）, VEGFR-2:8 nM （kd）, MEK-2:8300 nM （kd）, EPHA2:14 nM （kd）, CSF-1R:9 nM （kd）, Abl-1:3 nM （kd）, MEK-1:7100 nM （kd）, Lck:2 nM （kd）, RET:2 nM （kd）, c-Met:513 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 | CEP-32496 (hydrochloride), RXDX-105 hydrochloride |
| 分子量 | 553.92 |
| 分子式 | C24H23ClF3N5O5 |
| CAS No. | 1227678-26-3 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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