SNS-032 (BMS-387032)

製品コードS1145 バッチS114503

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₇H₂₄N₄O₂S₂

分子量

380.53

CAS No.

345627-80-7

Solubility (25°C)*

体外

DMSO

76 mg/mL (199.72 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）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	30%PEG400 1 0.5%Tween80 2 5%propylene glycol この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	30.000mg/ml (78.84mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. 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	SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. SNS-032 (BMS-387032) induces apoptosis.
in vitro	SNS-032 (BMS-387032) has low sensitivity to CDK1 and CDK4 with IC50 of 480 nM and 925 nM, respectively. This compound effectively kills chronic lymphocytic leukemia cells in vitro regardless of prognostic indicators and treatment history. Compared with flavopiridol and roscovitine, this agent is more potent, both in inhibition of RNA synthesis and at induction of apoptosis. Its activity is readily reversible; removal of this compound reactivates RNA polymerase II, which led to resynthesis of Mcl-1 and cell survival. ^[1] This inhibitor inhibits three dimensional capillary network formations of endothelial cells. It completely prevents U87MG cell–mediated capillary formation of HUVECs. In addition, this chemical significantly prevents the production of VEGF in both cell lines, it prevents in vitro angiogenesis, and this action is attributable to blocking of VEGF. Preclinical studies have shown that this compound induces cell cycle arrest and apoptosis across multiple cell lines. ^[2] This agent blocks the cell cycle via inhibition of CDKs 2 and 7, and transcription via inhibition of CDKs 7 and 9. Its activity is unaffected by human serum. ^[3] This compound induces a dose-dependent increase in annexin V staining and caspase-3 activation. At the molecular level, it induces a marked dephosphorylation of serine 2 and 5 of RNA polymerase (RNA Pol) II and inhibits the expression of CDK2 and CDK9 and dephosphorylated CDK7. ^[4]
in vivo	SNS-032 (BMS-387032) prevents tumor cell-induced VEGF secretion in a tumor coculture model. ^[2] This compound, a new CDK inhibitor, is more selective and less cytotoxic and has been shown to prolong stable disease in solid tumors. ^[4]

製品説明

SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. SNS-032 (BMS-387032) induces apoptosis.

in vitro

SNS-032 (BMS-387032) has low sensitivity to CDK1 and CDK4 with IC50 of 480 nM and 925 nM, respectively. This compound effectively kills chronic lymphocytic leukemia cells in vitro regardless of prognostic indicators and treatment history. Compared with flavopiridol and roscovitine, this agent is more potent, both in inhibition of RNA synthesis and at induction of apoptosis. Its activity is readily reversible; removal of this compound reactivates RNA polymerase II, which led to resynthesis of Mcl-1 and cell survival. ^[1]

This inhibitor inhibits three dimensional capillary network formations of endothelial cells. It completely prevents U87MG cell–mediated capillary formation of HUVECs. In addition, this chemical significantly prevents the production of VEGF in both cell lines, it prevents in vitro angiogenesis, and this action is attributable to blocking of VEGF. Preclinical studies have shown that this compound induces cell cycle arrest and apoptosis across multiple cell lines. ^[2]

This agent blocks the cell cycle via inhibition of CDKs 2 and 7, and transcription via inhibition of CDKs 7 and 9. Its activity is unaffected by human serum. ^[3]

This compound induces a dose-dependent increase in annexin V staining and caspase-3 activation. At the molecular level, it induces a marked dephosphorylation of serine 2 and 5 of RNA polymerase (RNA Pol) II and inhibits the expression of CDK2 and CDK9 and dephosphorylated CDK7. ^[4]

in vivo

SNS-032 (BMS-387032) prevents tumor cell-induced VEGF secretion in a tumor coculture model. ^[2]

This compound, a new CDK inhibitor, is more selective and less cytotoxic and has been shown to prolong stable disease in solid tumors. ^[4]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HUVECs and U87MG cells
	濃度	0–0.5 mM
	反応時間	24, 48, or 72 hours
	実験の流れ	Cell Titer-Glo (CTG) luminescent assay is performed to measure the growth curves of both HUVECs and U87MG cells. U87MG cells and HUVECs (2×10³ cells/well) are seeded in a 96-well microplate in a final volume of 100 ml. After 24 hours, cells are treated with various doses of SNS-032 (BMS-387032) for 24, 48, or 72 hours. After completion of the treatment, 100 ml of CTG solution is added to each well and incubated for 20 minutes at room temperature in the dark. Lysate (50 ml) is transferred to a 96-well white plate, and luminescence is measured by POLARstar OPTIMA. Percent cell growth is calculated by considering 100% growth at the time of this compound addition.
動物実験	動物モデル	Nude nu/nu BALB/c mice
	投薬量	15 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/19234140/
https://pubmed.ncbi.nlm.nih.gov/17534442/
https://pubmed.ncbi.nlm.nih.gov/19169685/

https://pubmed.ncbi.nlm.nih.gov/21212792/
https://pubmed.ncbi.nlm.nih.gov/22447844/

+ 展开

カスタマーフィードバック

: Data from [Data independently produced by Cell Death Differ, 2014, 21(3), 491-502]

: , , Dr. Yong-Weon Yi from Georgetown University Medical Center

: , , Yolanda Sanchez from Geisel School of Medicine at Dartmouth

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：

Combined therapy with DR5-targeting antibody-drug conjugate and CDK inhibitors as a strategy for advanced colorectal cancer [ Cell Rep Med, 2025, S2666-3791(25)00231-9]	PubMed: 40449480
SNS‑032 combined with decitabine induces caspase‑3/gasdermin E‑dependent pyroptosis in breast cancer cells [ Oncol Lett, 2025, 29(4):202]	PubMed: 40070781
Human Fallopian Tube-Derived Organoids with TP53 and RAD51D Mutations Recapitulate an Early Stage High-Grade Serous Ovarian Cancer Phenotype In Vitro [ Int J Mol Sci, 2024, 25(2)886]	PubMed: 38255960
Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin-dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology [ Elife, 2023, 12e88206]	PubMed: 37490324
Integrative analysis of drug response and clinical outcome in acute myeloid leukemia [ Cancer Cell, 2022, S1535-6108(22)00312-9]	PubMed: 35868306
Visual barcodes for clonal-multiplexing of live microscopy-based assays [ Nat Commun, 2022, 13(1):2725]	PubMed: 35585055
Systematic identification of biomarker-driven drug combinations to overcome resistance [ Nat Chem Biol, 2022, 10.1038/s41589-022-00996-7]	PubMed: 35332332
A SIX1 degradation inducer blocks excessive proliferation of prostate cancer [ Int J Biol Sci, 2022, 18(6):2439-2451]	PubMed: 35414775
Nuclear microRNAs release paused Pol II via the DDX21-CDK9 complex [ Cell Rep, 2022, 39(2):110673]	PubMed: 35417682
Co-targeting CDK2 and CDK4/6 overcomes resistance to aromatase and CDK4/6 inhibitors in ER+ breast cancer [ NPJ Precis Oncol, 2022, 6(1):68]	PubMed: 36153348

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。