Enitociclib (BAY 1251152)

Catalog No.S8730 Batch:S873001

Technical Data

Formula

C₁₉H₁₈F₂N₄O₂S

Molecular Weight

404.43

CAS No.

1610358-56-9

Solubility (25°C)*

In vitro

DMSO

81 mg/mL (200.28 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 Corn oil

4.25mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 85 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Enitociclib (BAY 1251152) is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins.

Targets

CDK9 ^[2]
(Cell-free assay)

3 nM

In vitro

BAY 1251152 (compound 2) significantly inhibits CDK9 and CDK2 with IC50 of 3 nM and 360 nM, respectively. BAY 1251152 (compound 2) shows cellular potency in MOLM13 with IC50 of 29 nM.^[1] ^[2]

In vivo

BAY 1251152 demonstrates excellent efficacy upon i.v. treatment in xenograft models (e.g. MOLM13) in mice and rats. BAY 1251152 is currently being evaluated in Phase I studies to determine the safety, tolerability, pharmacokinetics and initial pharmacodynamic biomarker response in patients with advanced cancer.^[2]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines HeLa, NCI-H460, A2780, DU 145, HeLa-MaTu-ADR, Caco-2, B16F10, MOLM-13 Concentrations 0.001 μM - 10 μM Incubation Time 4 days Method Cultivated tumour cells are plated in a 96-well multititer plate in 200 of their respective growth medium supplemented 10% fetal calf serum. After 24 hours, the cells of one plate (zero-point plate) are stained with crystal violet, while the medium of the other plates is replaced by fresh culture medium (200 μl ), to which the test substances are added in various concentrations (0 μM, as well as in the range of 0.001 -10 μM; the final concentration of the solvent dimethyl sulfoxide is 0.5%). The cells are incubated for 4 days in the presence of test substances.
Animal Study:^{^[2]}	Animal Models mice and rats with xenograft models (eg. MOLM13) Dosages -- Administration IV

Cell Assay:^{^[1]}

Cell lines
HeLa, NCI-H460, A2780, DU 145, HeLa-MaTu-ADR, Caco-2, B16F10, MOLM-13
Concentrations
0.001 μM - 10 μM
Incubation Time
4 days
Method
Cultivated tumour cells are plated in a 96-well multititer plate in 200 of their respective growth medium supplemented 10% fetal calf serum. After 24 hours, the cells of one plate (zero-point plate) are stained with crystal violet, while the medium of the other plates is replaced by fresh culture medium (200 μl ), to which the test substances are added in various concentrations (0 μM, as well as in the range of 0.001 -10 μM; the final concentration of the solvent dimethyl sulfoxide is 0.5%). The cells are incubated for 4 days in the presence of test substances.

Animal Study:^{^[2]}

Animal Models
mice and rats with xenograft models (eg. MOLM13)
Dosages
--
Administration
IV

References

Selleck's Enitociclib (BAY 1251152) has been cited by 6 publications

Androgen-repressed lncRNA LINC01126 drives castration-resistant prostate cancer by regulating the switch between O-GlcNAcylation and phosphorylation of androgen receptor [ Clin Transl Med, 2024, 14(1):e1531]	PubMed: 38214432
Synergistic Sensitization of High-Grade Serous Ovarian Cancer Cells Lacking Caspase-8 Expression to Chemotherapeutics Using Combinations of Small-Molecule BRD4 and CDK9 Inhibitors [ Cancers (Basel), 2023, 16(1)107]	PubMed: 38201534
Distinct patterns of RNA polymerase II and transcriptional elongation characterize mammalian genome activation [ Cell Rep, 2022, 41(13):111865]	PubMed: 36577375
The non-apoptotic function of Caspase-8 in negatively regulating the CDK9-mediated Ser2 phosphorylation of RNA polymerase II in cervical cancer [ Cell Mol Life Sci, 2022, 79(12):597]	PubMed: 36399280
Selective CDK9 Inhibition by Natural Compound Toyocamycin in Cancer Cells [ Cancers (Basel), 2022, 14(14)3340]	PubMed: 35884401
Recurrent Mutations in Cyclin D3 Confer Clinical Resistance to FLT3 Inhibitors in Acute Myeloid Leukemia [ Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3458]	PubMed: 34103301

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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