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CDKI-73

CAS No. : 1421693-22-2

MCE 站：CDKI-73

产品活性：CDKI-73 (LS-007) 是具有口服活性的、高效的 CDK9 抑制剂，其对CDK9、CDK1 和 CDK2 的 K_i 值分别为 4 nM、4 nM 和 3 nM。CDKI-73 可下调 RNA 聚合酶 II 的磷酸化。CDKI-73 也是一种 Rab11 的抑制剂。

研究领域：Cell Cycle/DNA Damage  |  Apoptosis

作用靶点：CDK  |  Apoptosis

In Vitro: CDKI-73 is highly cytotoxic to primary leukemia cells derived from CLL patients (mean LD₅₀ = 0.08 μM) and shows>500-fold selectivity for primary leukemia cells over normal B-lymphocytes (LD₅₀ = 40.5 μM).
CDKI-73 (0.1 μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells.
CDKI-73 induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II.
CDKI-73 is highly effective against all cell lines tested with an IC₅₀ in the range of 0.012-0.517 μM; in particular three MLL-AML cell lines, namely MOLM13, MV4-11 and THP-1, were highly sensitive to CDKI-73 with IC₅₀ values <0.062 μM.

In Vivo: CDKI-73 (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P < 0.001) without causing body weight loss and other overt toxicities..

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