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Alectinib

別名: AF-802, RG-7853,CH5424802 中文名稱：阿來替尼,艾樂替尼

Alectinib是一種有效的ALK抑制劑，在無細胞試驗中IC50為1.9 nM，對L1196M突變型敏感，對ALK比PF-02341066， NVP-TAE684和PHA-E429選擇性高。

Alectinib Chemical Structure

Alectinib Chemical Structure

CAS: 1256580-46-7

規(guī)格 價格 庫存 購買數(shù)量
5mg 1421.96 現(xiàn)貨
50mg 6315.15 現(xiàn)貨
1g 16134.3 現(xiàn)貨
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400-668-6834

info@selleck.cn
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Alectinib相關產(chǎn)品

相關信號通路圖

ALK Signaling Pathways

ALK信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
NIH/3T3 Antitumor assay 50 mg/kg 10 days Antitumor activity against mouse NIH/3T3 cells expressing EML4-ALK L1196M mutant xenografted in nude mouse assessed as tumor stasis at 50 mg/kg, po qd administered for 10 days 27131066
NIH/3T3 Antitumor assay 50 mg/kg 10 days Antitumor activity against mouse NIH/3T3 cells expressing EML4-ALK L1196M mutant xenografted in nude mouse assessed as partial tumor regression at 50 mg/kg, po qd administered for 10 days 27131066
MKN-45 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
NCI-H1993 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
NCI-H2009 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
Calu-1 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
NCI-H23 Growth inhibitory assay ~10 μM IC50=3600 nM 21575866
PC-1 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
Calu-3 Growth inhibitory assay ~10 μM IC50=>10,000 nM 21575866
NCI-H2228 Growth inhibitory assay ~10 μM IC50=53 nM 21575866
SK-N-FI Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
KELLY Growth inhibitory assay ~10 μM IC50=62 nM 21575866
NB-1 Growth inhibitory assay ~10 μM IC50=4.5 nM 21575866
HDLM-2 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
SR Growth inhibitory assay ~10 μM IC50=6.9 nM 21575866
KARPAS-299 Growth inhibitory assay ~10 μM IC50=3 nM 21575866
NCI-H2228 Kinase assay ~1 μM prevents autophosphorylation of ALK 21575866
SNU-5 Growth inhibitory assay ~10 μM IC50=1800 nM 21575866
KATO-III Growth inhibitory assay ~10 μM IC50=7900 nM 21575866
SK-BR-3 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
BT-483 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
PC-3 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
22Rv1 Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
U-87 MG Growth inhibitory assay ~10 μM IC50>10,000 nM 21575866
H3122 Growth inhibitory assay ~10 μM IC50=33 nM 25096400
LC-2/ad Apoptosis assay ~1 μM induces apoptosis 25349307
LC-2/ad Function assay ~1 μM inhibits the MAPK signaling pathway 25349307
Ba/F3 Function assay ~1 μM suppresses phosphorylation of ERK and increases the abundance of BIM 25349307
SNU-2535 Growth inhibitory assay ~10 μM IC50=33.1 nM 26849637
SNU-2535 Kinase assay ~1 μM inhibits the phosphorylation of ALK and its downstream molecules ERK1/2 and AKT 26849637
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.002 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.002 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.002 μM. 26568289
KARPAS299 Antiproliferative assay 96 hrs Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay, IC50 = 0.003 μM. 22225917
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.003 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.009 μM. 26568289
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.009 μM. 26568289
KARPAS299 Antiproliferative assay 72 hrs Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.015 μM. 27131066
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.0174 μM. 27131066
SUP-M2 Antiproliferative assay 72 hrs Antiproliferative activity against human SUP-M2 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.0179 μM. 27131066
NCI-H3122 Function assay 72 hrs Inhibition of ALK expressed in human NCI-H3122 cells assessed as cell growth inhibition after 72 hrs by SRB/CCK-8 assay, IC50 = 0.019 μM. 27131066
NCI-H3122 Antiproliferative assay 72 hrs Antiproliferative activity against ALK-dependent human NCI-H3122 cells after 72 hrs, IC50 = 0.019 μM. 26476749
SU-DHL1 Antiproliferative assay 72 hrs Antiproliferative activity against human SU-DHL1 cells after 72 hrs by SRB/CCK-8 assay, IC50 = 0.0205 μM. 27131066
NIH/3T3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse NIH/3T3 cells expressing wild type EML4-ALK after 72 hrs by SRB/CCK-8 assay, IC50 = 0.0323 μM. 27131066
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.072 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.09 μM. 26568289
NIH/3T3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse NIH/3T3 cells expressing EML4-ALK L1196 mutant after 72 hrs by SRB/CCK-8 assay, IC50 = 0.132 μM. 27131066
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.169 μM. 26568289
Ba/F3 Function assay 72 hrs Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay, IC50 = 0.207 μM. 26568289
DFCI114 Antiproliferative assay 72 hrs Antiproliferative activity against human DFCI114 cells expressing EML4-ALK G1269A mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.207 μM. 26568289
CHLA20 Antiproliferative assay 72 hrs Antiproliferative activity against human CHLA20 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.43 μM. 26568289
Kelly Antiproliferative assay 72 hrs Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.434 μM. 26568289
DFCI76 Antiproliferative assay 72 hrs Antiproliferative activity against human DFCI76 cells expressing EML4-ALK L1152R mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.511 μM. 26568289
LAN5 Antiproliferative assay 72 hrs Antiproliferative activity against human LAN5 cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.617 μM. 26568289
SMS-KCNR Antiproliferative assay 72 hrs Antiproliferative activity against human SMS-KCNR cells expressing EML4-ALK R1275Q mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.765 μM. 26568289
SK-N-SH Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-SH cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 0.872 μM. 26568289
SH-SY5Y Antiproliferative assay 72 hrs Antiproliferative activity against human SH-SY5Y cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.15 μM. 26568289
SK-N-BE(2) Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-BE(2) cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 1.554 μM. 26568289
LAN1 Antiproliferative assay 72 hrs Antiproliferative activity against human LAN1 cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 2.004 μM. 26568289
SK-N-AS Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-AS cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 2.139 μM. 26568289
SK-N-FI Antiproliferative assay 72 hrs Antiproliferative activity against human SK-N-FI cells expressing wild type EML4-ALK after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay, EC50 = 2.401 μM. 26568289
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生物活性

產(chǎn)品描述 Alectinib是一種有效的ALK抑制劑，在無細胞試驗中IC50為1.9 nM，對L1196M突變型敏感，對ALK比PF-02341066， NVP-TAE684和PHA-E429選擇性高。
靶點
ALK (F1174L) [1]
(Cell-free assay)		 ALK [1]
(Cell-free assay)		 ALK (R1275Q) [1]
(Cell-free assay)
1 nM 1.9 nM 3.5 nM
體外研究(In Vitro)
體外研究活性 CH5424802作用于ALK 為ATP競爭性的，解離常數(shù)(KD)為2.4 nM。CH5424802對ALK 和L1196M 具有強大的抑制效果，Ki分別為0.83 和1.56 nM。 CH5424802 作用于表達EML4-ALK的NCI-H2228 NSCLC細胞，抑制ALK自磷酸化。 CH5424802 也抑制STAT3 和AKT,而不是 ERK1/2的磷酸化。CH5424802 完全抑制STAT3在Tyr705位點的磷酸化。CH5424802優(yōu)先有效作用于表達EML4-ALK的 NCI-H2228細胞，而不作用于融合ALK的陰性 NSCLC細胞系，包括單層培養(yǎng)的HCC827細胞(EGFR外顯子19缺失), A549細胞(KRAS突變), 或NCI-H522細胞(EGFR 野生型, KRAS 野生型, 和ALK野生型)。CH5424802作用于 NCI-H2228球體細胞，引起凋亡標記—caspase-3/7樣激活。CH5424802抑制含NPM-ALK融合蛋白的兩種淋巴瘤細胞, KARPAS-299和SR生長,為不影響不含ALK融合的 HDLM-2淋巴瘤細胞生長。[1] CH5424802 作用于KARPAS-299具有高度靶向選擇性和更強的抗增殖活性。CH5424802抑制KAPRAS-299，IC50為3 nM, 抑制KDR， IC50為1.4 μM。CH5424802代謝穩(wěn)定性很高。[2]
激酶實驗 體外激酶抑制檢測
在CH5424802存在時，通過時間分辨熒光共振能量轉移（TR-FRET）分析或熒光偏振（FP）法測量磷酸化各種底物肽的能力，而測評抑制各種激酶（除了MEK1和 Raf-1）的能力。在CH5424802存在時，通過定量分析重組ERK2 蛋白對底物的磷酸化而測評對MEK1的抑制活性。在 CH5424802存在時，通過測定激酶磷酸化MEK1的能力而測評對Raf-1的抑制活性。
細胞實驗 細胞系 NSCLC, A549 和 HCC827 細胞
濃度 0-1 μM
孵育時間 5天
方法 NSCLC, A549 和HCC827細胞接種在96孔板中過夜，與不同濃度CH5424802按指定時間溫育。球體細胞生長抑制實驗中，細胞接種在球板上，溫育過夜，然后在指定時間用化合物處理。通過發(fā)光細胞活性檢測存活細胞。使用Caspase-Glo 3/7 檢測試劑盒進行Caspase-3/7檢測。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot pALK / ALK / pAKT / AKT / pERK / ERK / pS6 / S6

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