Signaling Pathway
重要通知：仅供研究使用。我们不向患者销售。
| Discription | Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively. | ||
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| Targets |
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| Cell Research |
[{"Cell Line": "BaF3", "Type": "IC50", "Value": "> 1000 nM", "Description": "Cytotoxicity against mouse BA/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "BaF3", "Type": "IC50", "Value": "169 nM", "Description": "Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "BaF3", "Type": "IC50", "Value": "2 nM", "Description": "Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "BaF3", "Type": "IC50", "Value": "2 nM", "Description": "Inhibition of EML4-ALK C1156Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "BaF3", "Type": "IC50", "Value": "2 nM", "Description": "Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "BaF3", "Type": "IC50", "Value": "207 nM", "Description": "Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "BaF3", "Type": "IC50", "Value": "3 nM", "Description": "Inhibition of EML4-ALK F1174L mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "BaF3", "Type": "IC50", "Value": "72 nM", "Description": "Inhibition of EML4-ALK 1151Tins mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "BaF3", "Type": "IC50", "Value": "9 nM", "Description": "Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "BaF3", "Type": "IC50", "Value": "90 nM", "Description": "Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse Ba/F3 cells assessed as cell viability after 72 hrs by MTS assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "KARPAS-299", "Type": "IC50", "Value": "15 nM", "Description": "Antiproliferative activity against human KARPAS299 cells after 72 hrs by SRB/CCK-8 assay", "Reference_Text": "[PMID: 27131066]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/27131066/"}, {"Cell Line": "KARPAS-299", "Type": "IC50", "Value": "3 nM", "Description": "Antiproliferative activity against human KARPAS-299 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay", "Reference_Text": "[PMID: 34402300]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/34402300/"}, {"Cell Line": "KARPAS-299", "Type": "IC50", "Value": "3 nM", "Description": "Antiproliferative activity against human KARPAS299 cells after 96 hrs by cell counting assay", "Reference_Text": "[PMID: 22225917]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/22225917/"}, {"Cell Line": "KARPAS-299", "Type": "IC50", "Value": "47 nM", "Description": "Antiproliferative activity against ALK-positive human KARPAS-299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay", "Reference_Text": "[PMID: 34176264]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/34176264/"}, {"Cell Line": "Kelly", "Type": "EC50", "Value": "434 nM", "Description": "Antiproliferative activity against human Kelly cells expressing EML4-ALK F1174L mutant after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay", "Reference_Text": "[PMID: 26568289]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/26568289/"}, {"Cell Line": "NB1", "Type": "IC50", "Value": "4.5 nM", "Description": "Antiproliferative activity against human NB1 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay", "Reference_Text": "[PMID: 34402300]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/34402300/"}, {"Cell Line": "NCI-H2228", "Type": "IC50", "Value": "53 nM", "Description": "Antiproliferative activity against human NCI-H2228 cells harbouring ALK by CellTiter-Glo luminescent cell viability assay", "Reference_Text": "[PMID: 34402300]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/34402300/"}, {"Cell Line": "NCI-H2228", "Type": "IC50", "Value": "6.5 nM", "Description": "Cytotoxicity in human NCI-H2228 cells harboring EML4-fused ALK variant 3 incubated for 72 hrs by alamar blue reagent based assay", "Reference_Text": "[PMID: 31425908]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/31425908/"}, {"Cell Line": "NCI-H3122", "Type": "IC50", "Value": "17.4 nM", "Description": "Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB/CCK-8 assay", "Reference_Text": "[PMID: 27131066]", "Reference_URL": "https://pubmed.ncbi.nlm.nih.gov/27131066/"}] |
| 目录号 | A18000 |
|---|---|
| 分子式 | C30H35ClN4O2 |
| 分子量 | 519.08 |
| CAS号 | 1256589-74-8 |
| SMILES | [H]Cl.N#CC1=CC2=C(C3=C(N2)C(C)(C4=CC(N5CCC(CC5)N6CCOCC6)=C(C=C4C3=O)CC)C)C=C1 |
| 其他名称 | CH5424802 Hydrochloride, CH 5424802, CH-5424802; RO5424802 Hydrochloride, RO 5424802, RO-5424802; AF-802 Hydrochloride, |
| 储存条件 | Store lyophilized at -20ºC, keep desiccated. |
| In vitro | DMSO | 2 mg/mL (3.85 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 19.26 mL | 96.32 mL | 192.65 mL |
| 0.5 mM | 3.85 mL | 19.26 mL | 38.53 mL |
| 1 mM | 1.93 mL | 9.63 mL | 19.26 mL |
| 5 mM | 0.39 mL | 1.93 mL | 3.85 mL |
Calculate the dilution required to prepare a stock solution. This equation is commonly abbreviated as: C1V1 = C2V2
