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HomeProduct name listSNS-032

SNS-032

SNS-032 Structural

What is SNS-032?

Description

Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. SNS-032 is an ATP-competitive inhibitor of Cdk9, 2, and 7 with IC50 values of 4, 38, and 62 nM, respectively. It is selective for these kinases and displays no additional activity against a panel of 190 kinases (IC50s = >1,000 nM). SNS-032 can block the cell cycle, inhibit transcription, and induce apoptosis in multiple myeloma RPMI-8226 cells with an IC90 value of 0.3 μM. This compound has been shown to induce apoptosis by inhibiting the transcription of the anti-apoptotic proteins, Mcl-1 and XIAP.

Chemical properties

Off-White Solid

The Uses of SNS-032

SNS 032 is a selective inhibitor of Cyclin-dependent Kinase (CDK) 2,7, and 9.

What are the applications of Application

SNS-032 is a potent and selective Cdk inhibitor

Definition

ChEBI: N-(5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-yl)piperidine-4-carboxamide is a secondary carboxamide resulting from the formal condensation of the carboxy group of piperidine-4-carboxylic acid with the amino group of 5-{[(5-tert-butyl-1,3-oxazol-2-yl)methyl]sulfanyl}-1,3-thiazol-2-amine. It is an ATP-competitive inhibitor of CDK2, CDK7 and CDK9 kinases and exhibits anti-cancer properties. It has a role as an apoptosis inducer, an antineoplastic agent, an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor and an angiogenesis inhibitor. It is a piperidinecarboxamide, a member of 1,3-oxazoles, a member of 1,3-thiazoles, an organic sulfide and a secondary carboxamide.

storage

Store at -20°C

References

[1]. tong w.g., chen r., plunkett w., et al. phase i and pharmacologic study of sns-032, a potent and selective cdk2, 7, and 9 inhibitor, in patients with advanced chronic lymphocytic leukemia and multiple myeloma. journal of clinical oncology, 2010, 28(18):3015- 3022.
[2]. chipumuro e., marco e., christensen c.l., et al. cdk7 inhibition suppresses super-enhancer-linked oncogenic transcription in mycn-driven cancer. cell, 2014, 159:1-14.
[3]. meng h., jin y.m., liu h., et al. sns-032 inhibits mtorc1/mtorc2 activity in acute myeloid leukemia cells and has synergistic activity with perifosine against akt. journal of hematology & oncology, 2013, 6:18.
[4]. chen r., wierda w.g., chubb s., et al. mechanism of action of sns032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. blood, 2009, 113(19):4637-4645.

Properties of SNS-032

Melting point: 171-173 °C
Density  1.28±0.1 g/cm3(Predicted)
storage temp.  under inert gas (nitrogen or Argon) at 2–8 °C
solubility  DMSO (Slightly), Methanol (Slightly)
form  Solid
pka 7.33±0.70(Predicted)
color  White to Off-White

Safety information for SNS-032

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for SNS-032

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