Basic information Safety Supplier Related

CEP-32496

Basic information Safety Supplier Related

CEP-32496 Basic information

Product Name:
CEP-32496
Synonyms:
  • CEP-32496
  • 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 hydrochloride
  • CEP-32496 (hydrochloride)
  • CEP32496 hydrochloride
  • CEP-32496 HCl salt
  • 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxaz
  • N-[3-[(6,7-Dimethoxy-4-quinazolinyl)oxy]phenyl]-N'-[5-(2,2,2-trifluoro-1,1-dimethylethyl)-3-isoxazolyl]urea hydrochloride
CAS:
1227678-26-3
MF:
C24H23ClF3N5O5
MW:
553.9181296
Mol File:
1227678-26-3.mol
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CEP-32496 Chemical Properties

storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Powder
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CEP-32496 Usage And Synthesis

Uses

CEP 32496 is an orally active BRAFV600E inhibitor with selective cellular and in vivo antitumor activity.

in vivo

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 (CEP-32496) 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 (CEP-32496) exhibits an exceptional PK profile in mouse, dog, and cynomolgus monkey. Administration of Agerafenib (CEP-32496) 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 (CEP-32496) (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)[1].

target

wild-type BRAF

IC 50

BRafV600E: 14 nM (Kd); Braf: 36 nM (Kd); CRAF: 39 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)

CEP-32496Supplier

China Langchem Inc.
Tel
0086-21-58956006
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
MedChemexpress LLC
Tel
021-58955995
Email
sales@medchemexpress.cn
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Email
info@adooq.com
CEG Chemical Science&Technology Co., Ltd.
Tel
Mobile:13665161512
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CEP-32496(1227678-26-3)Related Product Information