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Chemical Structure| 1610358-56-9 Chemical Structure| 1610358-56-9

Structure of Enitociclib
CAS No.: 1610358-56-9

Chemical Structure| 1610358-56-9

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(+)-BAY-1251152 is a CDK9 inhibitor, Phase 1 of Neoplasms.

Synonyms: (+)-VIP152; (+)-BAY-1251152; BAY 1251152

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Product Details of Enitociclib

CAS No. :1610358-56-9
Formula : C19H18F2N4O2S
M.W : 404.43
SMILES Code : N=S(CC1=CC(NC2=NC=C(F)C(C3=CC=C(F)C=C3OC)=C2)=NC=C1)(C)=O
Synonyms :
(+)-VIP152; (+)-BAY-1251152; BAY 1251152
MDL No. :MFCD31619237
InChI Key :YZCUMZWULWOUMD-UHFFFAOYSA-N
Pubchem ID :74767009

Safety of Enitociclib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Enitociclib

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
DLBCL cell lines 32-172 nM 6 hours Inhibited CDK9 phosphorylation, reduced expression of c-MYC, MCL-1, and cyclin D1, and induced caspase-3-dependent apoptosis Biomark Res. 2024 Jun 18;12(1):62.
MCL cell lines 32-172 nM 6 hours Inhibited CDK9 phosphorylation, reduced expression of c-MYC, MCL-1, and cyclin D1, and induced caspase-3-dependent apoptosis Biomark Res. 2024 Jun 18;12(1):62.
SU-DHL-10 cells 0.25 and1 μmol/L 4 hours Inhibition of RNA polymerase II Ser2 phosphorylation, leading to depletion of MYC and MCL1 mRNA and protein levels, and activation of apoptosis Cancer Res Commun. 2023 Nov 9;3(11):2268-2279.
SU-DHL-4 cells 0.25 and1 μmol/L 4 hours Inhibition of RNA polymerase II Ser2 phosphorylation, leading to depletion of MYC and MCL1 mRNA and protein levels Cancer Res Commun. 2023 Nov 9;3(11):2268-2279.
MOLM13 20 nmol/L to 1 μmol/L Continuous culture Establish BAY1251152-resistant cell line MOLM13-BR Acta Pharm Sin B. 2023 Sep;13(9):3694-3707.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NSG mice JeKo-1 cell line-derived xenografts (CDX) and patient-derived xenografts (PDX) Intravenous 10 mg/kg Twice a week Significantly inhibited tumor growth and prolonged mouse survival without significant body weight loss or other apparent adverse effects Biomark Res. 2024 Jun 18;12(1):62.
C.B-17 SCID mice SU-DHL-10 xenograft model Intravenously 10 and15 mg/kg Once weekly for 3 weeks 15 mg/kg dose induced complete tumor regression and observed depletion of MYC and MCL1 mRNA and protein levels, as well as activation of apoptosis Cancer Res Commun. 2023 Nov 9;3(11):2268-2279.
Balb/c nude mice MOLM13 and MOLM13-BR subcutaneous xenograft models Intravenous injection 8 mg/kg Every two days Evaluate the anti-tumor efficacy of BAY1251152 in resistant and non-resistant models Acta Pharm Sin B. 2023 Sep;13(9):3694-3707.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.36mL

2.47mL

1.24mL

24.73mL

4.95mL

2.47mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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