CEP-32496
- Product Name
- CEP-32496
- CAS No.
- 1227678-26-3
- Chemical Name
- CEP-32496
- Synonyms
- CEP-32496;CEP-32496 HCl salt;CEP-32496 USP/EP/BP;RXDX105 hydrochloride;CEP32496 hydrochloride;RXDX 105 hydrochloride;RXDX-105 hydrochloride;CEP 32496 hydrochloride;Agerafenib hydrochloride;CEP-32496 (hydrochloride)
- CBNumber
- CB82596590
- Molecular Formula
- C24H23ClF3N5O5
- Formula Weight
- 553.9181296
- MOL File
- 1227678-26-3.mol
CEP-32496 Property
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- C256693
- Product name
- CEP-32496Hydrochloride
- Packaging
- 10mg
- Price
- $385
- Updated
- 2021/12/16
- Product number
- 474082
- Product name
- CEP 32496
- Packaging
- 100mg
- Price
- $1890
- Updated
- 2021/12/16
- Product number
- 143691
- Product name
- 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride
- Purity
- 95%
- Packaging
- 1g
- Price
- $1998
- Updated
- 2021/12/16
- Product number
- 3015AH
- Product name
- 1-(3-((6,7-Dimethoxyquinazolin-4-yl)oxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)ureahydrochloride
- Packaging
- 1g
- Price
- $2747
- Updated
- 2021/12/16
- Product number
- 143691
- Product name
- 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride
- Purity
- 95%
- Packaging
- 5g
- Price
- $5994
- Updated
- 2021/12/16
CEP-32496 Chemical Properties,Usage,Production
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-32496 Preparation Products And Raw materials
Raw materials
Preparation Products
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