SNS-032 (BMS-387032) 345627-80-7

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Molecular Weight:

380.53 SNS-032 has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM 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.


Biological Activity


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. 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. 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. 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.


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



Protocol(Only for 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 (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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	380.53
Formula	C17H24N4O2S2
CAS No.	345627-80-7

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	76 mg/mL (199.72 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol	30 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.

Chemical Name	N-(5-((5-tert-butyloxazol-2-yl)methylthio)thiazol-2-yl)piperidine-4-carboxamide

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Product Categories : Cell Cycle > CDK Inhibitor