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MedChemExpress - Model Asnuciclib - ...

MedChemExpress - Model Asnuciclib - 1421693-22-2

Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion[1][2][3][4].

Asnuciclib

MCE China：Asnuciclib

Brand：MedChemExpress (MCE)

Cat. No.HY-12445

CAS：1421693-22-2

Synonyms：CDKI-73; LS-007

Purity：99.18%

Storage：4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Asnuciclib (CDKI-73; LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. Asnuciclib down-regulates the RNAPII phosphorylation. Asnuciclib is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion.

In Vitro：Asnuciclib 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)[1].Asnuciclib (0.1 μM, 4 h) inhibits the phosphorylation of serine 2 of RNA polymerase II and MCL1 protein expression in CLL cells[1].Asnuciclib induced caspase-dependent apoptosis that was preceded by dephosphorylation of cdk9 and serine 2 of RNA polymerase II[1].Asnuciclib 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 [3].

In Vivo：Asnuciclib (25, 50, 100 mg/kg) markedly decreases tumor growth in a dose-dependent manner and results in a prolongation of animal life span (P other overt toxicities.[3].

IC50 & Target：CDK2 3.27 nM (IC50) CDK9 5.78 nM (IC50) CDK1 8.17 nM (IC50) CDK4 8.18 nM (IC50) CDK6 37.68 nM (IC50) CDK7 134.26 nM (IC50) CDK1 4 nM (Ki) CDK2 3 nM (Ki) CDK9 4 nM (Ki) CDK7 91 nM (Ki)

References：

[1]. Lam F, et al. Targeting RNA transcription and translation in ovarian cancer cells with pharmacological inhibitor CDKI-73. Oncotarget. 2014 Sep 15;5(17):7691-704. [Content Brief]

[2]. Elisabeth Walsby, et al. A novel Cdk9 inhibitor preferentially targets tumor cells and synergizes with fludarabine. Oncotarget. 2014 Jan; 5(2): 375–385. [Content Brief]

[3]. Muhammed H Rahaman, et al. CDKI-73: an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia. Invest New Drugs. 2019 Aug;37(4):625-635. [Content Brief]

[4]. Alexandra Sorvina, et al. CDKI-73 is a Novel Pharmacological Inhibitor of Rab11 Cargo Delivery and Innate Immune Secretion. Cells. 2020 Feb 5;9(2):372. [Content Brief]

[5]. Shao Xie, et al. Antitumor action of CDK inhibitor LS-007 as a single agent and in combination with ABT-199 against human acute leukemia cells. Acta Pharmacol Sin. 2016 Nov; 37(11): 1481–1489. [Content Brief]

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