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CH5424802,艾乐替尼

CH5424802,艾乐替尼

规格或纯度: ≥98%

CAS编号: 1256580-46-7
分子式: C₃₀H₃₄N₄O₂
分子量: 482.62
PubChem编号: 49806720

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货号 (SKU)	包装规格	是否现货	价格	数量
C125242-5mg	5mg	现货
C125242-25mg	25mg	现货
C125242-100mg	100mg	现货
C125242-500mg	500mg	现货

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ALK receptor tyrosine kinase Inhibitor MET proto-oncogene，receptor tyrosine kinase Inhibitor

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基本描述

别名	艾乐替尼
英文别名	AF 802\|SR-01000389722-2\|9-ETHYL-6,6-DIMETHYL-8-[4-(MORPHOLIN-4-YL)PIPERIDIN-1-YL]-11-OXO-5H,6H,11H-BENZO[B]CARBAZOLE-3-CARBONITRILE\|9-Ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile\|Alectinib
规格或纯度	≥98%
英文名称	CH5424802
生化机理	CH5424802 is an ATP-competitive inhibitor for ALK and L1196M with Ki values of 0.83 nM and 1.56 nM, respectively. CH5424802 prevents autophosphorylation of ALK, and also suppresses the phosphorylation of STAT3 and AKT, but not of ERK1/2. CH5424802 elicits an apoptotic marker—caspase-3/7-like activation—in NCI-H2228 spheroid cells. CH5424802 blocks the growth of two NPM-ALK expressing lymphoma lines, KARPAS-299 and SR with greater efficacy against KARPAS-299 at an IC50 of 3 nM.
储存温度	-20°C储存
运输条件	超低温冰袋运输
产品介绍	Alectinib (CH5424802)是一种有效的ALK抑制剂，IC50为1.9 nM，对L1196M突变型敏感，作用于ALK比PF-02341066， NVP-TAE684和PHA-E429选择性高。An ATP-competitive inhibitor for ALK and L1196M. Alectinib (CH5424802) is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429 An ATP-competitive inhibitor for ALK and L1196M.

名称和标识符

IUPAC Name	9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
INCHI	InChI=1S/C30H34N4O2/c1-4-20-16-23-24(17-26(20)34-9-7-21(8-10-34)33-11-13-36-14-12-33)30(2,3)29-27(28(23)35)22-6-5-19(18-31)15-25(22)32-29/h5-6,15-17,21,32H,4,7-14H2,1-3H3
InChi Key	KDGFLJKFZUIJMX-UHFFFAOYSA-N
Canonical SMILES	CCC1=CC2=C(C=C1N3CCC(CC3)N4CCOCC4)C(C5=C(C2=O)C6=C(N5)C=C(C=C6)C#N)(C)C
Isomeric SMILES	CCC1=CC2=C(C=C1N3CCC(CC3)N4CCOCC4)C(C5=C(C2=O)C6=C(N5)C=C(C=C6)C#N)(C)C
PubChem CID	49806720
分子量	482.62

数据库链接

PubChem CID	49806720
ChEMBL Ligand	CHEMBL1738797
CAS Registry No.	1256580-46-7
RCSB PDB Ligand	EMH
PEP	alectinib
DrugCentral Ligand	4937

化学和物理性质

溶解性	DMSO ≥13mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL

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参考文献

1. Soda M, Choi YL, Enomoto M, Takada S, Yamashita Y, Ishikawa S, Fujiwara S, Watanabe H, Kurashina K, Hatanaka H et al.. (2007) Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer.. Nature, 448 (7153): (561-6). [PMID:17625570]
2. Takeuchi K, Choi YL, Togashi Y, Soda M, Hatano S, Inamura K, Takada S, Ueno T, Yamashita Y, Satoh Y et al.. (2009) KIF5B-ALK, a novel fusion oncokinase identified by an immunohistochemistry-based diagnostic system for ALK-positive lung cancer.. Clin Cancer Res, 15 (9): (3143-9). [PMID:19383809]
3. Sakamoto H, Tsukaguchi T, Hiroshima S, Kodama T, Kobayashi T, Fukami TA, Oikawa N, Tsukuda T, Ishii N, Aoki Y. (2011) CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.. Cancer Cell, 19 (5): (679-90). [PMID:21575866]
4. Kinoshita K, Asoh K, Furuichi N, Ito T, Kawada H, Hara S, Ohwada J, Miyagi T, Kobayashi T, Takanashi K et al.. (2012) Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802).. Bioorg Med Chem, 20 (3): (1271-80). [PMID:22225917]
5. Kodama T, Tsukaguchi T, Yoshida M, Kondoh O, Sakamoto H. (2014) Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance.. Cancer Lett, 351 (2): (215-21). [PMID:24887559]
6. Politi K, Gettinger S. (2014) Perfect ALKemy: optimizing the use of ALK-directed therapies in lung cancer.. Clin Cancer Res, 20 (22): (5576-8). [PMID:25228532]
7. Katayama R, Friboulet L, Koike S, Lockerman EL, Khan TM, Gainor JF, Iafrate AJ, Takeuchi K, Taiji M, Okuno Y et al.. (2014) Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib.. Clin Cancer Res, 20 (22): (5686-96). [PMID:25228534]

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