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P332+P313
피부 자극이 생기면 의학적인 조치· 조언을 구하시오.
P337+P313
눈에 대한 자극이 지속되면 의학적인 조치· 조언를 구하시오.
THAL-SNS-032 C화학적 특성, 용도, 생산
용도
THAL SNS 032 is a potent, selective and cereblon-dependent degrader of CDK9 (EC50 = 4 nM). Displays >15-fold selectivity for CDK9 over other CDKs (EC50 values are 62, 171 and 398 nM for CDK2, CDK1 and CDK7, respectively). Induces complete degradation of CDK9 at 250 nM in MOLT4 cells. Inhibits proliferation of leukemia cell lines.
생물학적 활성
THAL-SNS-032, a small molecule formed by conjugating the multi-targeting kinase inhibitor SNS-032 to thalidomide, induced potent and selective degradation of CDK9 in a CRBN-dependent fashion. Treatment with THAL-SNS-032 resulted in selective degradation of CDK9 with limited effects on the protein level of other CDKs. Furthermore, THAL-SNS-032 had a prolonged pharmacodynamic effect compared with traditional kinase inhibitors. The antitumoral activity of THAL-SNS-032 in cell lines expressing ER or both ER and HER2, including luminal A cells, has been demonstrated[1-2].