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CP-724714 Sale

(Synonyms: 2-甲氧基-N-[(2E)-3-[4-[[3-甲基-4-[(6-甲基-3-吡啶基)氧基]苯基]氨基]-6-喹唑啉基]-2-丙烯-1-基]乙酰胺) 目录号 : GC13091

A selective HER2/ErbB2 tyrosine kinase inhibitor

CP-724714 Chemical Structure

Cas No.:383432-38-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥725.00
现货
5mg
¥651.00
现货
25mg
¥2,342.00
现货
100mg
¥5,723.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

CP-724714 is an inhibitor of erbB2 and EGFR kinases with IC50 values of 10±3 nmol/L and 6,400±2,100 nmol/L, respectively [1].

In the in vitro cell cycle assay, CP-724714 cause a G1 block of the Her2-amplified BT-474 breast cancer cells due to its inhibition of erbB2. CP-724714 at 1 mol/L can also reduce the level of phospho-erbB2 in these cells. In in vivo assay, CP-724714 cause a concentration-dependent reduction of tumor erbB2 receptor phosphorylation in athymic mice bearing FRE-erbB2

Xenografts. CP-724714 treatments also resulted in a time- and dose-dependent induction of tumor cell apoptosis. In two human breast carcinoma models, BT-474 and MDA-MB-453, which are Her2 amplified and highly overexpress erbB2, CP-724714 is found to produce a dose-dependent inhibition of xenograft growth. In addition, CP-724,714 treatments induce reduction of downstream erbB2 RTK signaling. On the basis of these, CP-724,714 was advanced to phase I clinical trials and is potentially another option for Her2-driven breast cancer [1].

References:
[1] Jitesh P. Jani, Richard S. Finn, Mary Campbell, et al. Discovery and Pharmacologic Characterization of CP-724714, a Selective ErbB2 Tyrosine Kinase Inhibitor. Cancer Research. 2007 (67): 9887-9893.

Chemical Properties

Cas No. 383432-38-0 SDF
别名 2-甲氧基-N-[(2E)-3-[4-[[3-甲基-4-[(6-甲基-3-吡啶基)氧基]苯基]氨基]-6-喹唑啉基]-2-丙烯-1-基]乙酰胺
化学名 2-methoxy-N-[(E)-3-[4-[3-methyl-4-(6-methylpyridin-3-yl)oxyanilino]quinazolin-6-yl]prop-2-enyl]acetamide
Canonical SMILES CC1=NC=C(C=C1)OC2=C(C=C(C=C2)NC3=NC=NC4=C3C=C(C=C4)C=CCNC(=O)COC)C
分子式 C27H27N5O3 分子量 469.53
溶解度 ≥ 23.5mg/mL in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.1298 mL 10.6489 mL 21.2979 mL
5 mM 0.426 mL 2.1298 mL 4.2596 mL
10 mM 0.213 mL 1.0649 mL 2.1298 mL
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