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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 保质期:
Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
- 英文名:
CP724714
- 库存:
现询
- 供应商:
北京索莱宝科技有限公司
- CAS号:
383432-38-0
- 规格:
50mg/25mg/10mg/5mg/1mg
| 规格: | 50mg | 产品价格: | ¥4790.0 |
|---|---|---|---|
| 规格: | 25mg | 产品价格: | ¥2853.0 |
| 规格: | 10mg | 产品价格: | ¥1497.0 |
| 规格: | 5mg | 产品价格: | ¥827.0 |
| 规格: | 1mg | 产品价格: | ¥324.0 |
| 基本信息 | |
| CAS | No.383432-38-0 |
| 英文名称 | CP724714 |
| 分子式 | C27H27N5O3 |
| 分子量 | 469.54 |
| 溶解性 | Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Light yellow to yellow Solid |
| 储存条件 | Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year |
| MDL | MFCD11983048 |
| SMILES | CC1=NC=C(C=C1)OC2=C(C=C(C=C2)NC3=NC=NC4=C3C=C(C=C4)C=CCNC(=O)COC)C |
| InChIKey | LLVZBTWPGQVVLW-SNAWJCMRSA-N |
| InChI | InChI=1S/C27H27N5O3/c1-18-13-21(8-11-25(18)35-22-9-6-19(2)29-15-22)32-27-23-14-20(7-10-24(23)30-17-31-27)5-4-12-28-26(33)16-34-3/h4-11,13-15,17H,12,16H2,1-3H3,(H,28,33)(H,30,31,32)/b5-4+ |
| PubChem CID | 9874913 |
| 靶点 | HER2;ErbB2 |
| 通路 | Angiogenesis; Protein Tyrosine Kinase/RTK |
| 背景说明 | CP-724714 是HER2/ErbB2抑制剂。 |
| 生物活性 | CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities[1][2]. |
| In Vitro | CP-724714 is >1,000-fold less potent for insulin receptor, insulin-like growth factor-I receptor, platelet-derived growth factor β, vascular endothelial growth factor 2, Abl, Src, c-Met, JNK-2, JNK-3, ZAP-70, Cdk-2, and Cdk-5[1].CP-724714 potently reduces the EGF-induced autophosphorylation of the chimera containing the erbB2 kinase domain at a concentration as low as 50 nmol/L (IC50=32 nM) but is markedly less potent against EGFR[1].CP-724714 (1 μM; 24 hours) induces G1 cell cycle block in vitro in erbB2-overexpressing BT-474 human breast carcinoma cells[1].Cell Cycle Analysis[1]:Cell Line:erbB2-amplified BT-474 breast cancer cells;Concentration:1 μM;Incubation Time: 24 hours;Result:Resulted in accumulation of cells in G1 phase and a marked reduction in S-phase cells. |
| 细胞实验 | CP-724714 (3.25-100 mg/kg; p.o.; 0.5-8 hours) results in a concentration-dependent reduction of ErbB2 receptor phosphorylation[1].CP-724714 (6.25-100 mg/kg; p.o.; q.d; for 8 to 40 day) inhibits FRE-erbB2 xenograft growth[1].CP-724714 (Athymic, female FRE-erbB2 xenograft-bearing mice; 30 or 100 mg/kg; p.o.) treatments results in a time- and dose- dependent induction of apoptosis, which was evident as early as 4 to 8 h after dosing. Approximately 75% more tumor cells exhibited apoptotic changes in the 100 mg/kg treatment group compared with vehicle control group at 8 h after dosing. CP-724714 induces regression of BT-474 tumors and significant inhibition in a number of other human tumor xenografts. Additionally, CP-724714 showed a favorable nonclinical toxicity profile with no apparent effects on cardiac tissue[1].Animal Model:Female athymic mice (bearing FRE-erbB2 xenografts)[1];Dosage: 3.25-100 mg/kg;Administration:P.o.; 0.5-8 hours;Result:Produced a reduction of erbB2 tyrosine phosphorylation in FRE-erbB2 xenografts.Animal Model:Athymic female mice bearing FRE-erbB2 xenografts[1];Dosage: 6.25- 100 mg/kg;Administration:P.o.; q.d; for 8 to 40 day;Result:Resulted in an inhibition of FRE-erbB2 xenografts. |
| 数据来源文献 | [1]. Jani JP, et al. Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor. Cancer Res, 2007, 67(20), 9887-9893. [2]. Feng B, et al. Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714. Toxicol Sci, 2009, 108(2), 492-500. |
| 单位 | 瓶 |
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