- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實驗
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實驗
- Cell Counting Kit-8 (CCK-8)
- 新產(chǎn)品
- 聯(lián)系我們
Alectinib (CH5424802)
別名: AF-802, RG-7853,CH5424802
Alectinib是一種有效的ALK抑制劑，在無細(xì)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 (CH5424802) Chemical Structure
CAS: 1256580-46-7
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Alectinib (CH5424802)相關(guān)產(chǎn)品
| 相關(guān)產(chǎn)品 | TAE684 (NVP-TAE684) GSK1838705A Repotrectinib (TPX-0005) AZD3463 AP26113-analog (ALK-IN-1) ASP3026 Ensartinib dihydrochloride | 點擊展開 |
|---|---|---|
| 相關(guān)化合物庫 | 激酶抑制劑庫 酪氨酸激酶抑制劑分子庫 PI3K/Akt 抑制劑庫 細(xì)胞周期化合物庫 血管生成相關(guān)化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細(xì)胞實驗數(shù)據(jù)示例
| 細(xì)胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息(PMID) |
|---|---|---|---|---|---|
| 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 | |
| 點擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Alectinib是一種有效的ALK抑制劑，在無細(xì)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 |
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| 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(xì)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(xì)胞，而不作用于融合ALK的陰性 NSCLC細(xì)胞系，包括單層培養(yǎng)的HCC827細(xì)胞(EGFR外顯子19缺失), A549細(xì)胞(KRAS突變), 或NCI-H522細(xì)胞(EGFR 野生型, KRAS 野生型, 和ALK野生型)。CH5424802作用于 NCI-H2228球體細(xì)胞，引起凋亡標(biāo)記—caspase-3/7樣激活。CH5424802抑制含NPM-ALK融合蛋白的兩種淋巴瘤細(xì)胞, KARPAS-299和SR生長,為不影響不含ALK融合的 HDLM-2淋巴瘤細(xì)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(zhuǎn)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(xì)胞實驗 | 細(xì)胞系 | NSCLC, A549 和 HCC827 細(xì)胞 | ||||
| 濃度 | 0-1 μM | |||||
| 孵育時間 | 5天 | |||||
| 方法 | NSCLC, A549 和HCC827細(xì)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(xì)胞生長抑制實驗中，細(xì)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(xì)胞活性檢測存活細(xì)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(biāo) | 實驗圖片 | PMID | ||
| Western blot |
pALK / ALK / pAKT / AKT / pERK / ERK / pS6 / S6
| |||||