| CAS NO: | 2229037-04-9 |
| 规格: | ≥98% |
Molecular Formula: C45H53ClN10O10S MW: 961.48MW: 961.48 Solubility: Soluble to 100 mM in DMSO CAS No: 2229037-04-9 | |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Technical Information | Synonym: TL-1312; TL13-12; TL1312; TL13 12; Chemical Name: N-[2-[2-[2-[4-[4-[[5-Chloro-4-(2-propan-2-ylsulfonylanilino)pyrimidin-2-yl]amino]-3-methoxyphenyl]piperazin-1-yl]ethoxy]ethoxy]ethyl]-2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]acetamide InChi Key: WXNUIPVZMJMPNM-UHFFFAOYSA-N InChi Code: InChI=1S/C45H53ClN10O10S/c1-28(2)67(62,63)37-10-5-4-8-33(37)50-41-31(46)26-49-45(53-41)51-32-12-11-29(25-36(32)64-3)55-18-16-54(17-19-55)20-22-66-24-23-65-21-15-47-39(58)27-48-34-9-6-7-30-40(34)44(61)56(43(30)60)35-13-14-38(57)52-42(35)59/h4-12,25-26,28,35,48H,13-24,27H2,1-3H3,(H,47,58)(H,52,57,59)(H2,49,50,51,53) SMILES Code: O=C(NCCOCCOCCN1CCN(C2=CC=C(NC3=NC=C(Cl)C(NC4=CC=CC=C4S(=O)(C(C)C)=O)=N3)C(OC)=C2)CC1)CNC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O |
| Target | DC50 for degrading ALK: 10 and 180 nM[1] |
|---|---|
| In Vitro | TL13-12 (0-200 nM; 16 hours) is selective for degradation of ALK with the DC50s of 10 nM and 180 nM in H3122 cell and Karpas 299, respectively[1]. TL13-12 (0-160 nM; 16 hours) degrades ALK and aurora A protein expression as a dose-dependent manner in Kelly and CHLA20 cells[1]. TL13-12 (100 nM; 16 hours) significantly inhibits Tariqudan-induced ALK and Aurora A protein expression in CHLA20 cells[1]. Western Blot Analysis[1] Cell Line: Kelly and CHLA20 cells Concentration: 0 nM; 20 nM; 40 nM; 60 nM; 80 nM; 100 nM; 140 nM; 160 nM Incubation Time: 16 hours Result: Exhibited degrader behavior in cells. Western Blot Analysis[1] Cell Line: CHLA20 cells Concentration: 100 nM Incubation Time: 16 hours Result: Decreased ALK and Aurora A protein expression. |
| References | [1]. Powell CE, et al. Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).J Med Chem. 2018 May 10;61(9):4249-4255 |
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