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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
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C125242-5mg |
5mg |
现货 ![]() |
| |
C125242-25mg |
25mg |
现货 ![]() |
| |
C125242-100mg |
100mg |
现货 ![]() |
| |
C125242-500mg |
500mg |
现货 ![]() |
|
别名 | 艾乐替尼 |
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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 |
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 |
IUPAC Name | 9-ethyl-6,6-dimethyl-8-(4-morpholin-4-ylpiperidin-1-yl)-11-oxo-5H-benzo[b]carbazole-3-carbonitrile |
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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 |
PubChem CID | 49806720 |
分子量 | 482.62 |
PubChem CID | 49806720 |
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ChEMBL Ligand | CHEMBL1738797 |
CAS Registry No. | 1256580-46-7 |
RCSB PDB Ligand | EMH |
PEP | alectinib |
DrugCentral Ligand | 4937 |
溶解性 | DMSO ≥13mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
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输入批号以搜索COA:
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] |