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• 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。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *