卡奈替尼 (CI-1033)

规格或纯度: ≥98%

CAS编号: 267243-28-7
分子式: C₂₄H₂₅ClFN₅O₃
分子量: 485.94
PubChem编号: 156414

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货号 (SKU)	包装规格	是否现货
C125447-10mg	10mg	现货
C125447-50mg	50mg	现货
C125447-250mg	250mg	期货

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epidermal growth factor receptor Inhibitor erb-b2 receptor tyrosine kinase 2 Inhibitor

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基本描述

别名	PD-183805\|卡奈替尼\|卡耐替尼
英文别名	Canertinib\|267243-28-7\|CI-1033\|PD-183805\|Canertinib free base\|N-(4-(3-chloro-4-fluorophenylamino)-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\|N-[4-(3-c
规格或纯度	≥98%
英文名称	Canertinib (CI-1033)
生化机理	Canertinib is a potent and selective inhibitor of tyrosine residue phosphorylation of EGFR, blocking signal transgression and ceasing angiogenisis. Canertinib displays an IC50 = 1.5nM. Additionally, Canertinib’s action in inhibiting EGFR increases apoptosis in cancerous cell lines in a titratable fashion.
储存温度	-20°C储存
运输条件	超低温冰袋运输
备注	卖完停产，不再备货
产品介绍	Canertinib (CI-1033)是一种pan-ErbB抑制剂，同时抑制EGFR和ErbB2，IC50分别为1.5 nM和9.0 nM，但对PDGFR， FGFR， InsR， PKC，和CDK1/2/4等均无抑制活性。An irreversible pan-erbB tyrosine kinase inhibitor. Canertinib (CI-1033) 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. An irreversible pan-erbB tyrosine kinase inhibitor.

名称和标识符

IUPAC Name	N-[4-(3-chloro-4-fluoroanilino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]prop-2-enamide
INCHI	InChI=1S/C24H25ClFN5O3/c1-2-23(32)30-21-13-17-20(14-22(21)34-9-3-6-31-7-10-33-11-8-31)27-15-28-24(17)29-16-4-5-19(26)18(25)12-16/h2,4-5,12-15H,1,3,6-11H2,(H,30,32)(H,27,28,29)
InChi Key	OMZCMEYTWSXEPZ-UHFFFAOYSA-N
Canonical SMILES	C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
Isomeric SMILES	C=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
PubChem CID	156414
分子量	485.94

数据库链接

CAS Registry No.	267243-28-7
Wikipedia	Canertinib
DiscoveRx TREEspot	CI-1033\|
PubChem CID	156414
ChEMBL Ligand	CHEMBL31965
Reactome Reaction	R-HSA-1220611, R-HSA-1225978, R-HSA-9652264, R-HSA-9665121
Reactome Drug	R-ALL-1227677

CAS Registry No.

267243-28-7

Wikipedia

Canertinib

DiscoveRx TREEspot

CI-1033|

PubChem CID

156414

ChEMBL Ligand

CHEMBL31965

Reactome Reaction

R-HSA-1220611, R-HSA-1225978, R-HSA-9652264, R-HSA-9665121

Reactome Drug

R-ALL-1227677

溶解性	Soluble in DMSO (2 mg/ml), methanol, ethanol (9 mg/ml), and water (<1 mg/ml).

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参考文献

1. Smaill JB, Rewcastle GW, Loo JA, Greis KD, Chan OH, Reyner EL, Lipka E, Showalter HD, Vincent PW, Elliott WL et al.. (2000) 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, 43 (7): (1380-97). [PMID:10753475]
2. Rao GS, Murray S, Ethier SP. (2000) Radiosensitization of human breast cancer cells by a novel ErbB family receptor tyrosine kinase inhibitor.. Int J Radiat Oncol Biol Phys, 48 (5): (1519-28). [PMID:11121658]
3. Allen LF, Lenehan PF, Eiseman IA, Elliott WL, Fry DW. (2002) Potential benefits of the irreversible pan-erbB inhibitor, CI-1033, in the treatment of breast cancer.. Semin Oncol, 29 (3 Suppl 11): (11-21). [PMID:12138393]
4. Rixe O, Franco SX, Yardley DA, Johnston SR, Martin M, Arun BK, Letrent SP, Rugo HS. (2009) A randomized, phase II, dose-finding study of the pan-ErbB receptor tyrosine-kinase inhibitor CI-1033 in patients with pretreated metastatic breast cancer.. Cancer Chemother Pharmacol, 64 (6): (1139-48). [PMID:19294387]
5. Trinks C, Severinsson EA, Holmlund B, Gréen A, Gréen H, Jönsson JI, Hallbeck AL, Walz TM. (2011) The pan-ErbB tyrosine kinase inhibitor canertinib induces caspase-mediated cell death in human T-cell leukemia (Jurkat) cells.. Biochem Biophys Res Commun, 410 (3): (422-7). [PMID:21669187]
6. Nordigården A, Zetterblad J, Trinks C, Gréen H, Eliasson P, Druid P, Lotfi K, Rönnstrand L, Walz TM, Jönsson JI. (2011) Irreversible pan-ERBB inhibitor canertinib elicits anti-leukaemic effects and induces the regression of FLT3-ITD transformed cells in mice.. Br J Haematol, 155 (2): (198-208). [PMID:21848891]

卡奈替尼 (CI-1033)

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