CP-724714

产品名称：CP-724714

CP-724714生物活性：

CP-724,714 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. Phase 2. IC50 value: 10 nM 1 Target: HER2/ErbB2 in vitro: CP-724,714 is marked selectively against EGFR with IC50 of 6.4 μM. CP-724,714 is >1,000-fold less potent for IR, IGF-1R, PDGFRβ, VGFR2, abl. Src, c-Met c-jun NH2-terminal kinase (JNK)-2, JNK-3, ZAP-70, cyclin-dependent kinase (CDK)-2, and CDK-5. CP-724,714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain with IC50 of 32 nM, but is markedly less potent against EGFR in transfected NIH3T3 cells. CP-724,714 sensitively inhibits the proliferation of erbB2-amplified cells including BT-474 and SKBR3, with IC50 of 0.25 and 0.95 μM. CP-724,714 induces the accumulation of cells in G1 phase and a marked reduction in S-phase in BT-474 cells at 1 μM 1. CP-724,714 likely exerts its hepatotoxicity via both hepatocellular injury and hepatobiliary cholestatic mechanisms. CP-724,714 displays inhibition of cholyl-lysyl fluorescein and taurocholate (TC) efflux into canaliculi in cryopreserved and fresh cultured human hepatocytes, respectively. CP-724,714 inhibits TC transport in membrane vesicles expressing human bile salt export pump with IC50 of 16 μM and inhibits the major efflux transporter in bile canaliculi, MDR1, with IC50 of ~28 μM 2. in vivo: CP-724,714 (25 mg/kg) is rapidly absorbed after p.o. administration and causes reduction of tumor erbB2 receptor phosphorylation after dosing in FRE-erbB2 or BT-474 xenografts. CP-724,714 induces apoptosis in FRE-erbB2 xenograft–bearing (s.c.) mice and shows 50% tumor growth inhibition at 50 mg/kg, without weight loss or mortality. CP-724,714 also has great antitumor activity in MDA-MB-453, MDA-MB-231, LoVo (colon), and Colo-205 (colon) xenografts. Furthermore, CP-724,714 (30 or 100 mg/kg) reduces the extracellular signal–regulated kinase and Akt phosphorylation in BT-474 xenografts 1.

CP-724714制备储备液：

浓度溶解体积质量	1mg	5mg	10mg
1mM	2.1032mL	10.5159mL	21.0318mL
5mM	0.4206mL	2.1032mL	4.2064mL
10mM	0.2103mL	1.0516mL	2.1032mL
50mM	0.0421mL	0.2103mL	0.4206mL

CP-724714临床数据( 数据源于：http:// clinicaltrials.gov）

Conversion of different model animals based on BSA（Value based on data from FDA Draft Guidelines）


   Animal A (mg/kg)=Animal B（mg/kg）multiplied by    AnimalBm系数/AnimalAm系数
   For example, to modify the dose of resveratrol uesd for a mouse(22.4mg/kg) to a dose based on the BSA for a rat, multiply 22.4mg/kg by the Km factor for a mouse and zhen divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2mg/kg


   南京赛泓瑞生物科技有限公司是专业从事生化试剂、分子生物学试剂、实验耗材及实验仪器研发、销售、服务为一体的专业性生物科技公司。本着服务科学的理念，赛泓瑞建立了生命科学研究工具的研发、生产、销售及技术服务平台，现已有数万余种产品，并每年不断开发新产品，为广大的生命科学研究人员、医学、药学、农业、环保等的科研人员提供科研工具性产品及技术服务.
经营范围：抑制剂、ELISA试剂盒、原代细胞和细胞株、化学试剂、蛋白、抗体、分子试剂和试剂盒。