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CAS No.: 267243-28-7

Canertinib/卡奈替尼 Catalog No. CSN12261

Synonyms: CI-1033;PD-183805;卡奈替尼

Canertinib is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 EGFR

IC50:1.5nM HER2

IC50:9.0nM
描述Canertinib is a potent inhibitor of epidermal growth factor receptor (EGFR) with IC50 values of 7.4nM and 9nM for autophosphorylation of cellular EGFR and ErbB2, respectively^[3]. Canertinib inhibited the proliferation of melanoma cell lines RaH3 and RaH5 at 2-10µM after 72 hours of treatment. Canertinib at 1µM and 10µM also inhibited melanoma cell cycle progression and induced apoptosis, respectively, after 24 hours of treatment. The phosphorylation of ErbB1, ErbB2, and ErbB3 receptor in melanoma cells was inhibited by canertinib at a concentration of 1µM. Canertinib at 40 mg/kg/day (i.p. injection) significantly inhibited tumor growth in mice bearing human malignant melanoma xenografts within 18 days of treatment^[4].
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
A431 cells	-	Function assay	-	Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting, IC50=0.0074 μM	10753475
human A431 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTS assay, IC50=0.15 μM	22339342
human A431 cells	1 μM	Function assay	1 h	Irreversible inhibition of EGFR autophosphorylation in human A431 cells at 1 uM incubated for 1 hr followed by compound wash out measured 5 hrs post EGF addition by Western blotting analysis	24900594

更多
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00174356	Carcinoma, Non-Small Cell Lung	Phase 1	Completed	-	United States, Florida ... more >> Pfizer Investigational Site Tampa, Florida, United States, 33612 United States, Illinois Pfizer Investigational Site Park Ridge, Illinois, United States, 60068 Pfizer Investigational Site Skokie, Illinois, United States, 60076 United States, Kentucky Pfizer Investigational Site Louisville, Kentucky, United States, 40202 Pfizer Investigational Site Louisville, Kentucky, United States, 40207 United States, Texas Pfizer Investigational Site Houston, Texas, United States, 77030 Canada, Ontario Pfizer Investigational Site Hamilton, Ontario, Canada, L8V 5C2 Collapse <<
NCT00050830	Lung Neoplasms	Phase 2	Completed	-	-
NCT00051051	Breast Neoplasms	Phase 2	Completed	-	-

参考文献

[1] Nelson JM, Fry DW. Akt, MAPK (Erk1/2), and p38 act in concert to promote apoptosis in response to ErbB receptor family inhibition. J Biol Chem. 2001 May 4;276(18):14842-7.
[2] Smaill JB, Rewcastle GW, 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. 2000 Apr 6;43(7):1380-97.
[3] Smaill JB, Rewcastle GW, Loo JA, 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. 2000;43(7):1380-1397
[4] Djerf Severinsson EA, Trinks C, Gréen H, 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;414(3):563-568

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0579 mL
- 10.2894 mL
- 20.5787 mL
- 5 mM
- 0.4116 mL
- 2.0579 mL
- 4.1157 mL
- 10 mM
- 0.2058 mL
- 1.0289 mL
- 2.0579 mL

技术信息

CAS号

267243-28-7

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H25ClFN5O3

运输

蓝冰

分子量

485.94

别名

CI-1033;PD-183805;卡奈替尼;卡纳替尼

溶解度

DMSO	2.0 mg/mL (4.1 mM)
Water	Insoluble
Ethanol	9.0 mg/mL (18.5 mM)

动物实验配方

30% propylene glycol+5% Tween 80+65% water

10 mg/mL

suspension

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

A431 cells	-	Function assay	-	Inhibition of EGF-stimulated autophosphorylation of EGFR enzyme in A431 cells detected by immunoblotting, IC50=0.0074 μM	10753475
human A431 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A431 cells overexpressing EGFR after 72 hrs by MTS assay, IC50=0.15 μM	22339342
human A431 cells	1 μM	Function assay	1 h	Irreversible inhibition of EGFR autophosphorylation in human A431 cells at 1 uM incubated for 1 hr followed by compound wash out measured 5 hrs post EGF addition by Western blotting analysis	24900594
human A549 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A549 cells expressing wild type EGFR coexpressing k-Ras mutant after 72 hrs by MTS assay, IC50=1.59 μM	22339342
human BT474 cells	-	Proliferation assay	3 days	Antiproliferative activity against human BT474 cells overexpressing ERBb2 after 3 days by methylene blue staining, EC50=0.01 μM	19028424
human HCC827 cells	-	Proliferation assay	72 h	Antiproliferative activity against human HCC827 cells harboring EGFR del E746-A750 mutant after 72 hrs by MTS assay, IC50=0.001 μM	22339342
human HL7702 cells	-	Proliferation assay	72 h	Antiproliferative activity against human HL7702 cells expressing wilt type EGFR after 72 hrs by MTS assay, IC50=2.3 μM	22339342
human HN5 cells	-	Proliferation assay	3 days	Antiproliferative activity against human HN5 cells overexpressing EGFR after 3 days by methylene blue staining, EC50=0.05 μM	19028424
human LNCaP cells	10 μM	Function assay	2 h	Inhibition of autophosphorylation of immunoprecipitated flag-tagged Bmx expressed in human LNCaP cells assessed as incorporation of [32P]ATP at 10 uM pretreated for 2 hrs before transfection by immunoblot analysis	18667312
human NCI-H1975 cells	-	Proliferation assay	72 h	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTS assay, IC50=0.064 μM	22339342
MDA-MB 453 cells	-	Function assay	-	Inhibition of autophosphorylation of ERBB2 receptor kinase in MDA-MB 453 cells, IC50=0.009 μM	10753475
mouse BAF3 cells	-	Function assay	-	Inhibition of Blk expressed in mouse BAF3 cells assessed as cytotoxicity, IC50=0.029 μM	18667312
mouse BAF3 cells	-	Function assay	-	Inhibition of JAK3 expressed in mouse BAF3 cells assessed as cytotoxicity， IC50=2 μM	18667312
NCI-H1975 cells	-	Growth inhibition assay	48 h	Inhibition of EGFR L858R/T790M mutant in human NCI-H1975 cells assessed as growth inhibition after 48 hrs by MTT assay	24900594

靶点	Description	IC50
EGFR		IC50:1.5nM
HER2		IC50:9.0nM

Canertinib/卡奈替尼 Catalog No. CSN12261

靶点选择性

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