SNS-032 (BMS-387032)

Catalog No.S1145 Batch:S114501

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Technical Data

Formula

C17H24N4O2S2
Molecular Weight 380.53 CAS No. 345627-80-7
Solubility (25°C)* In vitro DMSO 76 mg/mL (199.72 mM)
Ethanol 30 mg/mL (78.83 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
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.
* <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 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. This compound induces apoptosis.
Targets
CDK9/CyclinT [3]
(Cell-free assay)		 CDK2/CyclinA [3]
(Cell-free assay)		 CDK2/CyclinE [1]
(Cell-free assay)		 CDK7/CyclinH [3]
(Cell-free assay)		 GSK-3α [3]
(Cell-free assay)		 View More
4 nM 38 nM 48 nM 62 nM 230 nM
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]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    HUVECs and U87MG cells

  • Concentrations

    0–0.5 mM

  • Incubation Time

    24, 48, or 72 hours

  • Method

    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.
Animal Study:

[5]
  • Animal Models

    Nude nu/nu BALB/c mice

  • Dosages

    15 mg/kg

  • Administration

    i.p.

References

  • 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/

Customer Product Validation

HeLa cells were treated for 3h with PIK-75 or SNS-032 at the indicated concentrations. Cells were subsequently lysed and subjected to western blotting. One representative of two independent experiments is shown.

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

<p>For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of SNS-032 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.</p><div><div> </div></div><p> </p>

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

, , Yolanda Sanchez from Geisel School of Medicine at Dartmouth

Efficacy of CDK9 inhibition in a syngeneic cancer model. Measurement of ascites fluid in the VEGF-DEF ID8 ovarian cancer mouse model is an indicator of tumor burden. In vivo treatment with the CDK9 inhibitor SNS-032 every 3 days demonstrated a decrease in tumor burden at weeks 4 and 5 (left). Addition of a-PD-1 led to a further decrease in tumor burden at week 5. Data are shown as mean + SEM (Mann-Whitney test). Survival of NSG mice was calculated using a log-rank (Mantel-Cox) test. MC180295 significantly extended survival of the mice in this model (right). In all panels, *p<0.05, **p < 0.01, ***p < 0.001. Bar graphs represent mean ± SD of at least biological triplicates.

Data from [ , , Cell, 2018, 175(5):1244-1258 ]

Selleck's SNS-032 (BMS-387032) Has Been Cited by 80 Publications

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

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