Enitociclib (BAY 1251152)

製品コードS8730 バッチS873001

印刷

化学情報

Synonyms

(+)-BAY-1251152

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₉H₁₈F₂N₄O₂S

分子量

404.43

CAS No.

1610358-56-9

Solubility (25°C)*

体外

DMSO

81 mg/mL (200.28 mM)

Water

Insoluble

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HeLa, NCI-H460, A2780, DU 145, HeLa-MaTu-ADR, Caco-2, B16F10, MOLM-13
	濃度	0.001 μM - 10 μM
	反応時間	4 days
	実験の流れ	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.
動物実験	動物モデル	mice and rats with xenograft models (eg. MOLM13)
	投薬量	--
	投与方法	IV

参考

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。