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CEP-32496

现货
Catalog No.
A1413
BRAF(V600E)抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,650.00
现货
5mg
¥ 1,450.00
现货
25mg
¥ 4,350.00
现货
100mg
¥ 9,800.00
现货

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Background

CEP-32496 is a highly potent and orally efficacious V600E mutant BRAF, WT BRAF and c-Raf inhibitor with Kd values of 14 nM, 36 nM and 39 nM, respectively.

In addition to BRAFV600E, CEP-32496 has exhibited high binding affinity for both wild-type BRAF and related CRAF, as well as certain receptor tyrosine kinases of known therapeutic utility, such as Abl-1, c-Kit, Ret, PDGFR-β, and VEGFR-2. However, CEP-32496 proved selective for the RAF members of the MAPK signal transduction pathway, as no significant affinity was observed for other key kinases of the MAPK pathway, including MEK-1, MEK-2, ERK-1, and ERK-2. This suggests that the observed cellular activity was driven primarily through inhibition of BRAFV600E, which is further supported by the observation that CEP-32496 exhibited selective cytotoxicity for tumor cell lines expressing mutant BRAF versus those expressing wild-type BRAF [1].

Oral administration of CEP-32496 to Colo-205 tumor xenograft-bearing mice resulted in significant inhibition of pMEK in tumor cell lysates [1].

References:
[1] Rowbottom MW1, Faraoni R, Chao Q, Campbell BT, Lai AG, Setti E, Ezawa M, Sprankle KG, Abraham S, Tran L, Struss B, Gibney M, Armstrong RC,Gunawardane RN, Nepomuceno RR, Valenta I, Hua H, Gardner MF, Cramer MD, Gitnick D, Insko DE, Apuy JL, Jones-Bolin S, Ghose AK, Herbertz T, Ator MA,Dorsey BD, Ruggeri B, Williams M, Bhagwat S, James J, Holladay MW. 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 oncogene homologue B1 (BRAF) V600E. J Med Chem. 2012 Feb 9;55(3):1082-105. doi: 10.1021/jm2009925. Epub 2012 Jan 23.

Chemical Properties

StorageStore at -20°C
M.Wt517.46
Cas No.1188910-76-0
FormulaC24H22F3N5O5
Solubility≥25.85mg/mL in DMSO
Chemical Name1-[3-(6,7-dimethoxyquinazolin-4-yl)oxyphenyl]-3-[5-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-3-yl]urea
SDFDownload SDF
Canonical SMILESCC(C)(C1=CC(=NO1)NC(=O)NC2=CC(=CC=C2)OC3=NC=NC4=CC(=C(C=C43)OC)OC)C(F)(F)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

CEP-32496