APS-2-79 hydrochloride
Cat. No.:YN350291
产品名称: | APS-2-79 hydrochloride |
CAS No.: | 2002381-31-7 |
Chemical Name: | 6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)-4-quinazolinamine, monohydrochloride |
Synonyms: | APS-2-79 (hydrochloride);APS 2-79 hydrochloride;6,7-Dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine hydrochloride;APS279 hydrochloride;BCP23567;s8355;AK685587;6,7-dimethoxy-N-(2-methyl-4-phenoxyphenyl)quinazolin-4-amine HCl;APS-2-79 hydrochloride |
分子量: | 423.9 |
分子式: | C23H21N3O3 • HCl |
SMILES: | COC1=C(OC)C=C(C(NC2=C(C)C=C(OC3=CC=CC=C3)C=C2)=NC=N4)C4=C1.Cl |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | APS-2-79 hydrochloride 是一种 KSR 依赖性的MEK拮抗剂。APS-2-79 与 ATPbiotin竞争性地结合到 KSR2-MEK1 复合物内的KSR2,IC50为 120 nM。APS-2-79 与 KSR 结合可将 KSR 固定在一个非活性的状态,使其无法再结合RAF和激活MEK,从而阻断了 Ras-MAPK 信号通路。 |
IC50和靶点: | [{name:"KSR2:120 nM (IC50)'}, 'MEK1'] |
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Dhawan, N.S., Scopton, A.P., and Arvin, C.D.Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signallingNature537(7618),112-116(2016)
Neilsen, B.K., Frodyma, D.E., Lewis, R.E., et al.KSR as a therapeutic target for Ras-dependent cancersExpert Opin. Ther. Targets.21(5),499-509(2017)