CPL304110

CAS: 1627826-19-0 货号: C655295 分子式: C25H30N6O2 分子量: 446.54
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
C655295-1ml
期货 Stock Image
¥2,420.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


CPL304110 is a potent, orally active and selective inhibitor of fibroblast growth factor receptors FGFR (1-3) , with IC 50 values of 0.75 nM, 0.5 nM, and 3.05 nM for FGFR (1-3), respectively

In Vitro

CPL304110 (0-0.6 μM) dose-dependently inhibits FGFR2 phosphorylation and downstream signaling (p-ERK). CPL304110 (compound 56q) exhibits in SNU-16 proliferation assay with an IC 50 of 85.64 nM. CPL304110 (compound 56q) demonstrats a more than 45-fold, 345-fold, 395-fold and 680-fold selectivity over KDR (VEGFR2), Flt3, Aura A and PDGFRb, respectively relative to FGFR2, and no significant inhibitory effects were observed with other tyrosine kinases. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: SNU-16 cell lines. Concentration: 0-0.6 μM. Incubation Time: 1 h. Result: Suppressed FGFR2 phosphorylation and downstream signaling (p-ERK)

In Vivo

CPL304110 (p.o., 40 mg/kg) exhibits a t 1/2 of 2 h and C max of 3369 ng/mL in mice . CPL304110 (compound 56q, 2 X 20 mg/kg) significantly inhibits tumor growth in mice without significant body loss or any toxicity. On day 21 (D21, day of termination) the tumor growth inhibition (TGI) is 64% for dosing 20 mg/kg twice a day . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Severe combined immunodeficient (SCID) mice implanted subcutaneously with SNU-16 (human) . Dosage: 20 mg/kg (X2). Administration: Orally, twice daily for 21 days. Result: After 6 hours of last dosing, concentration of 56q decreased in the plasma (9%) but increased stepwise in the tumor cells (121%).

IC50& Target:FGFR1 0.75 nM (IC 50 ) FGFR2 0.5 nM (IC 50 ) FGFR3 3.05 nM (IC 50 )

规格

规格或纯度
10mM in DMSO
英文名称
CPL304110
生化机理
CPL304110 是一种强效、口服活性和选择性的成纤维细胞生长因子受体 FGFR(1-3)抑制剂,对 FGFR(1-3)的 IC 50 值分别为 0.75 nM、0.5 nM 和 3.05 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
分子量
446.54

技术文档

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高级数据

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