Enitociclib

(+) -Enitociclib ((+) -BAY-1251152) is the enantiomer of Enitociclib (HY-103019E) with (+) optical rotation. Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies[1][2].

Product Specifications

CAS Number

[1610408-97-3]

Product Name Alternative

(+) -BAY-1251152; (+) -VIP152; (S) -Enitociclib

UNSPSC

12352005

Target

Apoptosis; CDK; DNA/RNA Synthesis; Drug Isomer

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Others

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/plus-enitociclib.html

Concentration

10mM

Purity

99.89

Solubility

DMSO : 113.3 mg/mL (ultrasonic; warming)

Smiles

COC1=C(C2=C(F)C=NC(NC3=CC(C[S@](C)(=N)=O)=CC=N3)=C2)C=CC(F)=C1

Molecular Formula

C19H18F2N4O2S

Molecular Weight

404.43

References & Citations

[1]Frigault MM, et al. Enitociclib, a Selective CDK9 Inhibitor, Induces Complete Regression of MYC+ Lymphoma by Downregulation of RNA Polymerase II Mediated Transcription. Cancer Res Commun. 2023 Nov 9;3 (11) :2268-2279.|[2]Tran S, et al. Enitociclib, a selective CDK9 inhibitor: in vitro and in vivo preclinical studies in multiple myeloma[J]. Blood Neoplasia, 2025, 2 (1) : 100050.