SNS-032 Chemical Properties

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

HS Code 

29349990

SNS-032 Usage And Synthesis

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

Uses

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

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.

SNS-032(345627-80-7)Related Product Information

• 3,3-Dimethyl-1-butyne
• N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)
• N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide hydrochloride
• N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea
• Y27632 (hydrochloride)
• Alisertib (MLN8237)
• PD 0332991 HCl
• (2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2-piperidineethanol
• Flavopiridol (Alvocidib) HCl
• Olaparib
• Hexahydroisonicotinamide
• 1-BOC-PIPERIDINE-4-CARBOXYLIC ACID [5-(5-TERT-BUTYL-OXAZOL-2-YLMETHYLSULFANYL)-THIAZOL-2-YL]-AMIDE
• SNS-032