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CH5424802,艾乐替尼

规格或纯度: ≥98%
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ALK receptor tyrosine kinase Inhibitor MET proto-oncogene，receptor tyrosine kinase Inhibitor
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基本描述

规格或纯度 ≥98%
英文名称 CH5424802
别名 艾乐替尼
英文别名 AF-802;CH 5424802;CH-5424802;AF802;AF 802; Alectinib; 9-Ethyl-6,11-dihydro-6,6-dimethyl-8-[4-(4-morpholinyl)-1-piperidinyl]-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
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
分子式

C30H34N4O2
PubChem CID 49806720
分子量 482.62

化学和物理性质

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

靶标

Target ID 1815
名称 MET proto-oncogene, receptor tyrosine kinase
缩写名 MET
家族 Type X RTKs: HGF (hepatocyte growth factor) receptor family
别名 Mas-related G-protein coupled receptor member X1
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 1390 7q31 MET MET proto-oncogene, receptor tyrosine kinase
Mouse 1 1379 6 7.83 cM Met met proto-oncogene
Rat 1 1382 4q21 Met MET proto-oncogene, receptor tyrosine kinase
Ensembl Gene ENSG00000105976 (Hs) , ENSMUSG00000009376 (Mm) , ENSRNOG00000052745 (Rn)
Entrez Gene 17295 (Mm) , 4233 (Hs)
OMIM 164860 (Hs)
Protein GI 188595716 (Hs) , 146198696 (Mm) , 13629392 (Rn)
UniProtKB P08581 (Hs) , P16056 (Mm) , P97523 (Rn)
RefSeq Nucleotide NM_000245 (Hs) , NM_008591 (Mm) , NM_031517 (Rn)
RefSeq Protein NP_000236 (Hs) , NP_032617 (Mm) , NP_113705 (Rn)
Orphanet 123201 (Hs)
DrugBank Target P08581 (Hs)
CATH/Gene3D 2.130.10.10 (N/A) , 2.60.40.10 (N/A)
ChEMBL Target CHEMBL3717 (Hs) , CHEMBL5585 (Mm)
Target ID 1839
名称 ALK receptor tyrosine kinase
缩写名 ALK
家族 Type XIX RTKs: Leukocyte tyrosine kinase (LTK) receptor family
别名 Mrgprc11
基因和蛋白信息
Species Transmembrane Domains Amino Acids Chromosomal Location Gene Symbol Gene Name
Human 1 1620 2p23.2-p23.1 ALK ALK receptor tyrosine kinase
Mouse 1 1621 17 43.77 cM Alk anaplastic lymphoma kinase
Rat 2 1617 6q13 Alk ALK receptor tyrosine kinase
Ensembl Gene ENSG00000171094 (Hs) , ENSMUSG00000055471 (Mm) , ENSRNOG00000008683 (Rn)
Entrez Gene 11682 (Mm) , 238 (Hs)
OMIM 105590 (Hs)
Protein GI 29029632 (Hs) , 110347475 (Mm)
UniProtKB P97793 (Mm) , Q9UM73 (Hs)
RefSeq Nucleotide NM_001169101 (Rn) , NM_004304 (Hs) , NM_007439 (Mm)
RefSeq Protein NP_001162572 (Rn) , NP_004295 (Hs) , NP_031465 (Mm)
Orphanet 160020 (Hs)
DrugBank Target Q9UM73 (Hs)
ChEMBL Target CHEMBL4247 (Hs) , CHEMBL5771 (Mm)

关联配体

Ligand ID 7739
名称 alectinib
别名 CH5424802
类别 Synthetic organic
学名 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile
生物活性评价 Alecitinib has potent anti-tumour effects in crizotinib resistant cells, in in vivo xenograft models .
评价 Alectinib is a second generation ALK inhibitor. It was developed to inhibit the expression of the mutated ALK gene that causes growth of some non-small cell lung cancers, in patients whose cancer has become resistant to the older ALK inhibitor, . However, additional mutations may develop which confer alecitinib resistance . Cells harbouring these novel mutations are reported to be sensitive to and other next-generation ALK tyrosine kinase inhibitors . The identification of the mechanisms by which acquired tumour resistance occurs highlights the importance of being able to use the correct drug for the correct patient to maximise the clinical benefit
The design and synthesis of alectinib (CH5424802) is described in .

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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