| 产品描述： | Agerafenib (CEP-32496; RXDX-105) is a highly potent and orally efficacious inhibitor of BRAFV600E with a Kd of 14 nM. |
| 靶点： |
Braf:36 nM (Kd);CRAF:39 nM (Kd);BRafV600E:14 nM (Kd);c-Kit:2 nM (Kd);Ret:2 nM (Kd);LCK:2 nM (Kd);Abl-1:3 nM (Kd);VEGFR-2:8 nM (Kd);CSF-1R:9 nM (Kd);EPHA2:14 nM (Kd);EGFR:22 nM (Kd);c-Met:513 nM (Kd);JAK-2:4700 nM (Kd);MEK-1:7100 nM (Kd);MEK-2:8300 nM (Kd);Raf;c-RET;Bcr-Abl;PDGFR;Src;c-Kit |
| 体内研究： |
Oral administration of Agerafenib (CEP-32496) to Colo-205 tumor xenograft-bearing mice results in significant inhibition of pMEK in tumor cell lysates. For instance, a single 30 mg/kg (po) dose of Agerafenib leads to a 50 and 75% inhibition of normalized pMEK in tumor lysates at the 2 and 6 h postdose time point, respectively (p<0.03), while a 55 mg/kg (po) dose resulted in a 75% to 57% (p<0.03) inhibition of pMEK at 2 through 10 h post administration, with normalization to baseline by 24 h. Agerafenib exhibits an exceptional PK profile in mouse, dog, and cynomolgus monkey. Administration of Agerafenib to beagle dogs (single dose of 1 mg/kg iv and 10 mg/kg po) 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 iv and 10 mg/kg po) leads to high oral exposure due to low clearance (CL=6.7 mL/min/kg) and excellent bioavailability (%F=100) |
| 参考文献： |
1. Rowbottom MW, et al. Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral on |
| 溶解性： |
DMSO : 50 mg/mL (96.63 mM; Need ultrasonic) |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.933 ml |
9.663 ml |
19.325 ml |
| 5 mM |
0.387 ml |
1.933 ml |
3.865 ml |
| 10 mM |
0.193 ml |
0.966 ml |
1.933 ml |
| 50 mM |
0.039 ml |
0.193 ml |
0.387 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京