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: Cat #: V3570 CAS #: 2229037-04-9 Purity ≥ 98%
Description: TL13-12 is novel, potent and selective PROTAC degrader of anaplastic lymphoma kinase (ALK) with potential anticancer activity. It degrades ALK with DC50 values of 10 and 180 nM in H3122 and Karpas 299 cells, respectively. It comprises the cereblon E3 ligase ligand Pomalidomide conjugated to an ALK inhibitor. TL13-12 is the first small molecule degraders that can induce anaplastic lymphoma kinase (ALK) degradation, including in non-small-cell lung cancer (NSCLC), anaplastic large-cell lymphoma (ALCL), and neuroblastoma (NB) cell lines. TL13-12 was developed through conjugation of known pyrimidine-based ALK inhibitors, TAE684 or LDK378, and the cereblon ligand pomalidomide. In some cell types, the degrader potency is compromised by expression of drug transporter ABCB1. In addition, proteomic profiling demonstrated that these compounds also promote the degradation of additional kinases including PTK2 (FAK), Aurora A, FER, and RPS6KA1 (RSK1).
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| CAS No. | 2229037-04-9 |
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| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent |
| Protocol | 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. |
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This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.