2-Methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]acetamide
- CAS No.383432-38-0
- Chemical Name:2-Methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]acetamide
- CBNumber:CB92484874
- Molecular Formula:C27H27N5O3
- Formula Weight:469.54
- MOL File:383432-38-0.mol
- Boiling point 687.3±55.0 °C(Predicted)
- Density 1.251
- storage temp. Store at -20°C
- solubility DMF: 3 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml; DMSO: 3 mg/ml; Ethanol: 2 mg/ml
- form A crystalline solid
- pka 13.95±0.46(Predicted)
- color Light yellow to yellow
- FDA UNII I05QZ0S4V3
- UNSPSC Code 12352200
- NACRES NA.77
-
Symbol(GHS)
- Signal wordWarning
- Hazard statements H302
- Precautionary statements P280-P305+P351+P338
- Brand: Sigma-Aldrich(India)
- Product number: PZ0335
- Product name : CP724714
- Purity: ≥98% (HPLC)
- Packaging: 5MG
- Price: ₹10954.9
- Updated: 2022/06/14
- Buy: Buy
- Brand: Sigma-Aldrich(India)
- Product number: PZ0335
- Product name : CP724714
- Purity: ≥98% (HPLC)
- Packaging: 25MG
- Price: ₹44057.75
- Updated: 2022/06/14
- Buy: Buy
2-Methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]acetamide Chemical Properties,Usage,Production
- Description CP 724,714 is a selective inhibitor of HER2/ErbB2 with an IC50 value of 10 nM. It demonstrates greater than 640-fold selectivity against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, Abl, Src, and c-Met. CP 724,714 has been shown to inhibit the proliferation of ErbB2-amplified cells, including BT474 and SK-BR-3 with IC50 values of 0.25 and 0.95 μM, respectively. It also demonstrates antitumor activity in various human tumor xenograft models. However, CP 724,714 was discontinued from clinical development due to hepatotoxicity caused by its ability to inhibit hepatic efflux transporters at low micromolar concentrations.
- Uses CP 724714 is a HER-2 tyrosine kinase inhibitor used in tumor treatments for HER2 positive solid tumors.
- Definition ChEBI: CP-724714 is a 2-methoxy-N-[3-[4-[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]anilino]-6-quinazolinyl]prop-2-enyl]acetamide in which the double bond adopts a trans-configuration. It is a potent inhibitor of HER2/ErbB2 (IC50 = 10 nM) and exhibits anti-cancer activity. It has a role as an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an antineoplastic agent, an apoptosis inducer and a hepatotoxic agent.
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in vivo
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. - IC 50 ErbB2: 10 nM (IC50)
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- 信号转导通路激酶抑制剂
- 合成有机化合物配体
- 抑制剂
- 蛋白酪氨酸激酶
- 化合物CP724714,10 MM DMSO 溶液
- CP-724714,ERBB2抑制剂
- (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
- 化合物CP724714
- 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
- 383432-38-0
- CP-724714, 10 mM in DMSO
- CP-724714(b)
- Acetamide, 2-methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]-
- CP 724714;CP724714;CP-724714 (E-DOUBLE BOND)
- CP 724714 NEW
- CS-2306
- CP-724;714;CP724;714;CP 724714;CP 724;714;CP724714;CP-724714
- CP-724
- CP724
- CP 724
- 714
- (E)-2-Methoxy-N-(3-(4-(3-methyl-4-(6-methylpyridin-3-yloxy)phenylamino)quinazolin-6-yl)allyl)a
- CP-724714(E)-2-methoxy-N-(3-(4-(3-methyl-4-(6-methylpyridin-3-yloxy)phenylamino)quinazolin-6-yl)allyl)acetamide
- CP-724714 (E-Double bond)
- 2-Methoxy-N-[(2E)-3-[4-[[3-Methyl-4-[(6-Methyl-3-pyridinyl)oxy]phenyl]aMino]-6-quinazolinyl]-2-prope
- 2-Methoxy-N-[(2E)-3-[4-[[3-methyl-4-[(6-methyl-3-pyridinyl)oxy]phenyl]amino]-6-quinazolinyl]-2-propen-1-yl]acetamide