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Canertinib

(Synonyms: 卡奈替尼; CI-1033; PD-183805)

目录号: PL08119 纯度: ≥99%

Canertinib (CI-1033;PD-183805) 是有效的，不可逆的 EGFR 抑制剂；抑制细胞 EGFR 和 ErbB2 自身磷酸化的 IC50 值分别为 7.4 和 9 nM。Canertinib 可以用于研究小鼠的牛痘病毒呼吸道感染。

CAS No. :267243-28-7

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中文名称	Canertinib
中文别名	卡奈替尼;卡耐替尼;卡奈替尼卡那替尼;卡纽替尼;卡奈替尼(双盐);卡拉替尼;卡奈替尼Canertinib 卡纽替尼CI-1033
英文名称	Canertinib
英文别名	Canertinib;CI-1033;PD-183805;N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide;N-[4-(3-chloro-4-fluoro-anilino)-7-(3-morpholinopropoxy)quinazolin-6-yl]acrylamide;CI-1033(Canertinib);Canertinib base;Canetinib;Canertinib (CI-1033);N-[4-(3-chloro-4-fluoroanilino)-7-(3-Morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-en;2-Propenamide,N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazoliny...;2-Propenamide,N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-;Canertinib (CI-1033,CI 1033, PD-183805, PD-0183805);N-(4-(3-Chloro-4-fluorophenylamino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamide;UNII-C78W1K5ASF;N-[4-(3-Chloro-4-fluoroanilino)-7-(3-morpholinopropoxy)quinazolin-6-yl]acrylamide;N-{4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(morpholin-4-yl)propoxy]quinazolin-6-yl}prop-2-enamide;C78W1K5ASF;CI1033;PD183805;N-(4-((3-chloro-4-fluorophenyl)amino)-7-(3-morpholinopropoxy)quinazolin-6-yl)acrylamide;N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(3-(morpholin-4-yl)prop
Cas No.	267243-28-7
分子式	C₂₄H₂₅ClFN₅O₃
分子量	485.94
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Canertinib (CI-1033;PD-183805) 是有效的，不可逆的 EGFR 抑制剂；抑制细胞 EGFR 和 ErbB2 自身磷酸化的 IC50 值分别为 7.4 和 9 nM。Canertinib 可以用于研究小鼠的牛痘病毒呼吸道感染。

产品详情

Canertinib (CI-1033;PD-183805) 是有效的，不可逆的 EGFR 抑制剂；抑制细胞 EGFR 和 ErbB2 自身磷酸化的 IC₅₀ 值分别为 7.4 和 9 nM。Canertinib 可以用于研究小鼠的牛痘病毒呼吸道感染。

生物活性

Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC 50 s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice.

性状

Solid

IC50 & Target[1][2]

EGFR 7.4 nM (IC50) ErbB2 9 nM (IC50

体外研究(In Vitro)

Canertinib significantly inhibits growth of cultured melanoma cells, RaH3 and RaH5, in a dose-dependent manner. IC50 is approximately 0.8 μM and by 5μM both cell lines are completely growth-arrested within 72 h of treatment. Incubation of exponentially growing RaH3 and RaH5 with 1 μM canertinib accumulated the cells in the G1-phase of the cell cycle within 24 h of treatment without induction of apoptosis. 1 μM canertinib inhibits ErbB1-3 receptor phosphorylation with a concomitant decrease of Akt-, Erk1/2- and Stat3 activity in both cell lines.
Canertinib also is a potent activator of exosome secretion.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Canertinib shows superior in vivo antitumor activity, giving growth delays in A431 xenografts exceeding 50 days following oral administration. The growth of human malignant melanoma xenografts, RaH3 and RaH5, in nude mice is significantly inhibited by i.p. injections of 40 mg/kg/day canertinib (Fig. 4). The anti-proliferative effect on melanoma xenografts is visible already within 4 days of treatment and further increased throughout the treatment period as observed through the differences in tumor volumes, reaching statistical significance within 18 days of treatment. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Smaill JB, et al. Tyrosine kinase inhibitors. 17. Irreversible inhibitors of the epidermal growth factor receptor: 4-(phenylamino)quinazoline- and 4-(phenylamino)pyrido[3,2-d]pyrimidine-6-acrylamides bearing additional solubilizing functions. J Med Chem.
[2]. Djerf Severinsson EA, et al. The pan-ErbB receptor tyrosine kinase inhibitor canertinib promotes apoptosis of malignant melanoma in vitro and displays anti-tumor activity in vivo. Biochem Biophys Res Commun. 2011 Oct 28;414(3):563-8.

溶解度数据	In Vitro: Ethanol : 12.5 mg/mL (25.72 mM; Need ultrasonic)DMSO : 4.9 mg/mL (10.08 mM; Need warming)配制储备液

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Data Sheet

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Canertinib

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