首页
应用
药物靶标
激酶
TK：酪氨酸激酶
来那替尼 (HKI-272), 受体蛋白-酪氨酸激酶 erbB-4 抑制剂

来那替尼 (HKI-272), 受体蛋白-酪氨酸激酶 erbB-4 抑制剂

规格或纯度: ≥99%

CAS编号: 698387-09-6
分子式: C₃₀H₂₉ClN₆O₃
分子量: 557.04
PubChem编号: 9915743

有货

库存信息

关闭

库存信息

关闭

库存信息

关闭

货号 (SKU)	包装规格	是否现货
N126132-5mg	5mg	现货
N126132-25mg	25mg	现货
N126132-100mg	100mg	期货

Skip to the end of the images gallery

Skip to the beginning of the images gallery

基本描述

别名	来那替尼
英文别名	EC 244-343-6\|N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)butanamide\|CHEBI:61397\|N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide\|NERATIN
规格或纯度	≥99%
英文名称	Neratinib (HKI-272)
生化机理	Neratinib is a potent and selective inhibitor of EGFR and Neu(HER2) (IC50 = 92 nM and 59 nM, respectively) by preventing phosphorylation of these proteins by their respective kinases. Neratinib displays activity against a variety of cancer cell lines, including A431, 3T3, and MDA-MB-435. Neratinib is an inhibitor of c-Src and Flk-1.
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	Neratinib (HKI-272)是一种高度选择性的HER2和EGFR抑制剂，IC50分别为59 nM和92 nM；微弱抑制KDR和Src，对Akt，CDK1/2/4， IKK-2， MK-2， PDK1， c-Raf和c-Met没有显著的抑制作用。Phase 3。A potent and selective inhibitor of EGFR and HER2 Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3. A potent and selective inhibitor of EGFR and HER2

ALogP	4.9

名称和标识符

IUPAC Name	(E)-N-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide
INCHI	InChI=1S/C30H29ClN6O3/c1-4-39-28-16-25-23(15-26(28)36-29(38)9-7-13-37(2)3)30(20(17-32)18-34-25)35-21-10-11-27(24(31)14-21)40-19-22-8-5-6-12-33-22/h5-12,14-16,18H,4,13,19H2,1-3H3,(H,34,35)(H,36,38)/b9-7+
InChi Key	JWNPDZNEKVCWMY-VQHVLOKHSA-N
Canonical SMILES	CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CCN(C)C
Isomeric SMILES	CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)/C=C/CN(C)C
PubChem CID	9915743
分子量	557.04

数据库链接

CAS Registry No.	698387-09-6
Wikipedia	Neratinib
DiscoveRx TREEspot	HKI-272\|
PubChem CID	9915743
ChEMBL Ligand	CHEMBL180022
Reactome Reaction	R-HSA-1220611, R-HSA-1225978, R-HSA-9652264, R-HSA-9665412, R-HSA-9665121, R-HSA-9665702, R-HSA-9665286
Reactome Drug	R-ALL-1216527
DrugCentral Ligand	5252

CAS Registry No.

698387-09-6

Wikipedia

Neratinib

DiscoveRx TREEspot

HKI-272|

PubChem CID

9915743

ChEMBL Ligand

CHEMBL180022

Reactome Reaction

R-HSA-1220611, R-HSA-1225978, R-HSA-9652264, R-HSA-9665412, R-HSA-9665121, R-HSA-9665702, R-HSA-9665286

Reactome Drug

R-ALL-1216527

DrugCentral Ligand

5252

化学和物理性质

溶解性	Soluble in DMSO (2 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).

相关文档

产品问答

登录提交问题

查看全部

您提交该产品问题后,我们会在1-2个工作日内给您答复,您可以登录"我的账号",然后点击"我的产品问答"查看答案

参考文献

1. Rabindran SK, Discafani CM, Rosfjord EC, Baxter M, Floyd MB, Golas J, Hallett WA, Johnson BD, Nilakantan R, Overbeek E et al.. (2004) Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase.. Cancer Res, 64 (11): (3958-65). [PMID:15173008]
2. Park JW, Liu MC, Yee D, Yau C, van 't Veer LJ, Symmans WF, Paoloni M, Perlmutter J, Hylton NM, Hogarth M et al.. (2016) Adaptive Randomization of Neratinib in Early Breast Cancer.. N Engl J Med, 375 (1): (11-22). [PMID:27406346]

来那替尼 (HKI-272), 受体蛋白-酪氨酸激酶 erbB-4 抑制剂

库存信息

库存信息

库存信息

基本描述

产品属性

名称和标识符

数据库链接

化学和物理性质

质检证书(COA)

质检报告(COA)

相关文档

质检报告COA

产品问答

产品问答

参考文献