Asnuciclib

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].

Product Specifications

CAS Number

[1421693-22-2]

Product Name Alternative

CDKI-73; LS-007

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Apoptosis; CDK

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/asnuciclib.html

Purity

99.76

Solubility

DMSO : ≥ 52 mg/mL

Smiles

CNC1=NC(C)=C(C2=C(F)C=NC(NC3=CC(S(=O)(N)=O)=CC=C3)=N2)S1

Molecular Formula

C15H15FN6O2S2

Molecular Weight

394.45

Precautions

H302, H315, H319

References & Citations

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