2. Cell Cycle/DNA Damage
    Apoptosis
  3. CDK
    Apoptosis
  4. SNS-032

SNS-032  (Synonyms: BMS-387032)

Cat. No.: HY-10008 Purity: 99.49%
COA Handling Instructions

SNS-032 (BMS-387032) est un inhibiteur puissant et sélectif des CDK2, CDK7 et CDK9 avec IC50 de 38 nM, 62 nM et 4 nM, respectivement. SNS-032 a un effet antitumoral.

SNS-032 (BMS-387032) ist ein potenter und selektiver Inhibitor von CDK2, CDK7, und CDK9 mit IC50s von 38 nM, 62 nM bzw. 4 nM. SNS-032 hat eine antitumorale Wirkung.

SNS-032 (BMS-387032) is a potent and selective inhibitor of CDK2, CDK7, and CDK9 with IC50s of 38 nM, 62 nM and 4 nM, respectively. SNS-032 has antitumor effect.

For research use only. We do not sell to patients.

SNS-032 Chemical Structure

SNS-032 Chemical Structure

CAS No. : 345627-80-7

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Solution
10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 61 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 55 In-stock
Estimated Time of Arrival: December 31
10 mg USD 77 In-stock
Estimated Time of Arrival: December 31
50 mg USD 165 In-stock
Estimated Time of Arrival: December 31
100 mg USD 275 In-stock
Estimated Time of Arrival: December 31
200 mg USD 495 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK

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  • Customer Review

Description

SNS-032 (BMS-387032) is a potent and selective inhibitor of CDK2, CDK7, and CDK9 with IC50s of 38 nM, 62 nM and 4 nM, respectively. SNS-032 has antitumor effect[1].

IC50 & Target

CDK9

4 nM (IC50)

CDK2

38 nM (IC50)

CDK7

62 nM (IC50)

CDK1

480 nM (IC50)

CDK4

925 nM (IC50)

In Vitro

SNS-032 has low sensitivity to CDK1 and CDK4 with IC50 of 480 nM and 925 nM, respectively. SNS-032 effectively kills chronic lymphocytic leukemia cells in vitro regardless of prognostic indicators and treatment history. Compared with flavopiridol and roscovitine, SNS-032 is more potent, both in inhibition of RNA synthesis and at induction of apoptosis. SNS-032 activity is readily reversible; removal of SNS-032 reactivates RNA polymerase II, which led to resynthesis of Mcl-1 and cell survival[1]. SNS-032 inhibits three dimensional capillary network formations of endothelial cells. SNS-032 completely prevents U87MG cell–mediated capillary formation of HUVECs. In addition, SNS-032 significantly prevents the production of VEGF in both cell lines, SNS-032 prevents in vitro angiogenesis, and this action is attributable to blocking of VEGF. Preclinical studies have shown that SNS-032 induces cell cycle arrest and apoptosis across multiple cell lines[2]. SNS-032 blocks the cell cycle via inhibition of CDKs 2 and 7, and transcription via inhibition of CDKs 7 and 9. SNS-032 activity is unaffected by human serum[3]. SNS-032 induces a dose-dependent increase in annexin V staining and caspase-3 activation. At the molecular level, SNS-032 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[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

SNS-032 (15 mg/kg, i.p.) inhibits both xenografted BaF3-T674I cells and KBM5-T315I cells in vivo. SNS-032 abrogates the growth of tumors transplanted in nude mice with downregulation of T674I PDGFRα and T315I-Bcr-Abl[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

380.53

Appearance

Solid

Formula

C17H24N4O2S2
CAS No.
SMILES

CC(C)(C1=CN=C(CSC2=CN=C(NC(C3CCNCC3)=O)S2)O1)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (164.24 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6279 mL 13.1396 mL 26.2791 mL
5 mM 0.5256 mL 2.6279 mL 5.2558 mL
10 mM 0.2628 mL 1.3140 mL 2.6279 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.47 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.49%

COA (246 KB) HNMR (255 KB) LCMS (267 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

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 (0-0.5 mM) 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 SNS-032 addition.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

Nude nu/nu BALB/c mice are housed in barrier facilities with a 12-hour light-dark cycle, with food and water available ad libitum. A mixture of 1×107 of BaF3-T674I cells with Matrigel or KBM5-T315I cells (3×107) are inoculated subcutaneously on the flanks of 4- to 6-week-old male nude mice. Tumors are measured every other day with use of calipers. Tumor volumes are calculated by the following formula: a2×b×0.4, where a is the smallest diameter and b is the diameter perpendicular to a. Four days after subcutaneous inoculation, when tumors are palpable (appr 100 mm3), mice are randomized to receive treatment with vehicle (tissue culture medium containing DMSO 0.1% v/v) or SNS-032 (15 mg/kg injected intraperitoneally every 2 days) for about 2 weeks. SNS-032 is dissolved in tissue culture grade DMSO before dilution. The body weight, feeding behavior, and motor activity of each animal are monitored as indicators of general health. The animals are then euthanized, and tumor xenografts are immediately removed, weighed, stored, and fixed.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

SNS-032345627-80-7BMS-387032SNS032SNS 032BMS387032BMS 387032CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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