SNS-032 (BMS-387032)

Catalog No.S1145

Molecular Weight(MW): 380.53

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. Phase 1.

3 Customer Reviews

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.

Dr. Yong-Weon Yi from Georgetown University Medical Center. SNS-032 (BMS-387032) purchased from Selleck.

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.

Cell Death Differ 2014 21(3), 491-502. SNS-032 (BMS-387032) purchased from Selleck.
Yolanda Sanchez from Geisel School of Medicine at Dartmouth. SNS-032 (BMS-387032) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description

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	View More

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. ^[4]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
human A2780 cell line	MmWzVJJwdGmoZYLheIlwdiCjc4PhfS=>	MmnrO\|IhcA>?	M3vSVmFvfGmycn;sbYZmemG2aY\lJIVn\mWldDDh[4FqdnO2IHj1cYFvKEF{N{iwJINmdGxibHnu[UB4[XNiZHX0[ZJucW6nZDDpckBiKHeqb3zlJINmdGxiN{KgbJIh[3m2b4TvfIlkcXS7IHHzd4F6NCCLQ{WwQVk2KG6P	NWL5ZVRkOTVyMke4OlM>
human HCT116 cells	NUfsTJRSTnWwY4Tpc44h[XO\|YYm=		M2j5PWlvcGmkaYTpc44hd2ZiQ1TLPUBqdiCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgdIhwe3Cqb4Ktd4VzOiCuZY\lcEBw\iCUTlGgdI9tgW2ncnHz[UAzKGGodHXyJFE3KGi{czDifUBpcWeqIHPvcpRmdnRiY3XscJVt[XJiYYPzZZktKEmFNUC9OFU5KG6P	MX6xPFg1OjRyOR?=
human HCT116 cells	MYjGeY5kfGmxbjDhd5NigQ>?	MYSxOkBp	MlrCTY5pcWKrdHnvckBw\iCFRFu5MY1m\GmjdHXkJHJPSSCyb3ygNkBxcG:\|cHjvdplt[XSrb36gZZQhe2W{MjDpckBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgNVYhcHK\|IHL5JGhEWyCjc4PhfUwhUUN3ME2wMlU2KM7:TR?=	NYfpcW5NOTh7Mk[2PVk>

... Click to View More Cell Line Experimental Data

In vivo

SNS-032 prevents tumor cell-induced VEGF secretion in a tumor coculture model. ^[2] SNS-032, a new CDK inhibitor, is more selective and less cytotoxic and has been shown to prolong stable disease in solid tumors. ^[4]

Protocol

Cell Research:^[2]	+ Expand 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 (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. (Only for Reference)

Cell Research:^[2]

+ Expand

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 (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.
(Only for Reference)

References

[4] Walsby E, et al. Leukemia, 2011, 25(3), 411-9.

+ Expand

Solubility (25°C)

In vitro	DMSO	76 mg/mL (199.72 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% PEG400+0.5% Tween80+5% propylene glycol For best results, use promptly after mixing.	30 mg/mL

* 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.

Chemical Information Download SNS-032 (BMS-387032) SDF

Molecular Weight	380.53
Formula	C₁₇H₂₄N₄O₂S₂
CAS No.	345627-80-7
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00446342	Completed	B-lymphoid Malignancies\|Chronic Lymphocytic Leukemia\|Mantle Cell Lymphoma\|Multiple Myeloma	Sunesis Pharmaceuticals	February 2007	Phase 1
NCT00292864	Completed	Tumors	Sunesis Pharmaceuticals	January 2006	Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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CDK Signaling Pathway Map

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Ro-3306 ^New

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases.
Purvalanol A ^New

Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively.
Palbociclib (PD-0332991) HCl

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

Features:Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
Palbociclib (PD0332991) Isethionate

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Flavopiridol HCl

Flavopiridol HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.
Roscovitine (Seliciclib,CYC202)

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SNS-032 (BMS-387032)