|(E)-2-甲氧基-N-(3-(4-((3-甲基-4-((6-甲基吡啶-3-基)氧基)苯基)氨基)喹唑啉-6-基)烯丙基)乙酰胺|CsnPharm

CAS No.: 383432-38-0

CP-724714 Catalog No. CSN18252

Synonyms: CP 724,714;CP-724714(E-Double Bond)

CP-724714 is a potent, selective inhibitor of HER2/ErbB2 with IC50 of 10 nM, > 640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, c-Met etc.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 HER2

IC50:10nM
描述Human epidermal growth factor receptor (EGFR; HER1,erbB1), human epidermal growth factor r eceptor 2 (HER2; erbB2), HER3 (erbB3) and HER4 (erbB4) are members of the ErbB family of transmembrane receptor tyrosine kinases. Among them, HER2 is a validated and high-value target. Approximately 30% of breast cancers have an amplification of the HER2/neu gene or overexpression of its protein product, HER2. Also, overexpression of HER2 occurs in gastric, colorectal, NSCLC and ovarian cancers. CP-724714 is a potent inhibitor of HER2 with IC50 value of 10nM (measured by kinase activity), ~640-fold selectivity for HER2 than the closely related kinase EGFR. NIH 3T3 cells transfected with chimeric EGFR/HER2 exposure to CP-724714>250nM showed decrease of EGF-induced autophosphorylation level of HER2. Colony formation was reduced by >80% by CP-724714 at concentration of 1μM in BT-474 cells and at 3μM in SKBR3 cells. Accumulation in G1 phase and a marked reduction in S-phase can be observed in BT-474 cells treated with 1μM CP-724714 for 24h. Oral administration of CP-724714 at dose ranging in 6.25-100mg/kg, q.d., resulted in dose-dependent inhibition of FRE-erbB2 xenografts and 50% tumor growth inhibition at 50mg/kg. Tumor growth inhibition by 41%, 42%, 81% and 100% achieved by 1, 10, 30, and 100 mg/kg CP-724714 in BT-474 xenografts. Also, the tumor growth inhibition of MDA-MB-453 xenografts by 19%, 66%, and 83% was achieved in the 25, 50 and 100 mg/kg b.i.d. treatment groups, respectively. Meanwhile, the reduction ranging in 69%-79% of HER2 phosphorylation in these groups treated with CP-724714 can be observed. Also, treatment with CP-724714 at 30mg/kg or 100mg/kg resulted in significant reduction of p-ERK and p-ATK, the downstreams activated by HER2, in BT-474 xenografts^[1].
动物研究
剂量
Mice^[1] (p.o.): min = 3.125 mg/kg, max = 100 mg/kg

给药途径
p.o.
临床研究

动物研究
剂量	Mice^[1] (p.o.): min = 3.125 mg/kg, max = 100 mg/kg
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00055926	Breast Cancer	Phase 1	Completed	-	United States, California ... more >> Jonsson Comprehensive Cancer Center, UCLA Los Angeles, California, United States, 90095-1781 Collapse <<
NCT00102895	Breast Neoplasms ... more >> Neoplasm Metastasis Collapse <<	Phase 2	Terminated(See Detailed Descri... more >>ption) Collapse <<	-	-

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1298 mL
- 10.6488 mL
- 21.2977 mL
- 5 mM
- 0.4260 mL
- 2.1298 mL
- 4.2595 mL
- 10 mM
- 0.2130 mL
- 1.0649 mL
- 2.1298 mL

技术信息

CAS号

383432-38-0

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H27N5O3

运输

蓝冰

分子量

469.54

别名

CP 724,714;CP-724714(E-Double Bond)

溶解度

DMSO	50.0 mg/mL (106.5 mM)

动物实验配方

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