TL12-186

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TL12-186 是一种依赖于 Cereblon 的多激酶 PROTAC 降解剂。包括 CDK，BTK，FLT3，Aurora激酶，TEC，ULK，ITK 等。TL12-186 抑制 CDK2/cyclin A 和 CDK9/cyclin T1，IC50 分别为 73 和 55 nM。

TL12-186 is a Cereblon-dependent multi-kinase PROTAC degrader. Multi-kinases include CDK, BTK, FLT3, Aurora kinases, TEC, ULK, ITK, et al. TL12-186 inhibits CDK2/cyclin A (IC50=73 nM) and CDK9/cyclin T1 (IC50=55 nM).

Cell Proliferation Assay Cell Line:WT and CRBN-/- MOLM-14 cells; WT and CRBN-/- MOLT-4 cells Concentration:1, 10, 100, 1000, 10000 nM Incubation Time:2 days Result:Exhibited a CRBN-dependent pharmacological effect, displaying 13 to 15-fold more potent inhibition of survival of the WT cells than the CRBN-/- cells.Western Blot Analysis Cell Line:MOLT-4 cells Concentration:10, 100, 1000, 10000 nM Incubation Time:4 hours Result:Inhibited IFN-γ (10 ng/mL)-stimulated STAT1 phosphorylation (Y701) without causing degradation of JAK1 or JAK2.

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Others

Other Targets

PROTACs | CDK

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2250025-88-6

931.46

C44H51ClN10O9S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 200 mg/mL (214.72 mM; 超声助溶 )

O=C1NC(=O)C(N2C(=O)C=3C=CC=C(NCC(=O)NCCOCCOCCN4CCN(C5=CC=C(C=C5)NC6=NC=C(Cl)C(=N6)NC=7C=CC=CC7S(=O)(=O)C(C)C)CC4)C3C2=O)CC1

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(-20℃)

With Ice Pack

≥ 2 years