345627-80-7 Usage
Uses
Used in Pharmaceutical Industry:
N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide is used as a selective inhibitor for Cyclin-dependent Kinase (CDK) 2, 7, and 9. It is particularly effective in cancer therapy, as CDKs are key regulators of cell cycle progression, making them promising targets for cancer treatment. N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide is an ATP-competitive inhibitor with IC50 values of 4, 38, and 62 nM for Cdk9, 2, and 7, respectively. It selectively inhibits these kinases without additional activity against a panel of 190 kinases (IC50s > 1,000 nM). By blocking the cell cycle, inhibiting transcription, and inducing apoptosis in cancer cells, N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide has the potential to be a valuable therapeutic agent in the fight against cancer.
Used in Drug Development:
In the drug development industry, N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide can be utilized as a lead compound for the development of novel therapeutics targeting CDKs. Its selective inhibition of CDK 2, 7, and 9, along with its ability to induce apoptosis by inhibiting the transcription of anti-apoptotic proteins, makes it a promising candidate for further research and development into potential cancer treatments.
Used in Research and Development:
In the research and development sector, N-[5-[(5-tert-butyl-1,3-oxazol-2-yl)methylsulfanyl]-1,3-thiazol-2-yl]piperidine-4-carboxamide can be employed as a tool compound to study the role of CDKs in cell cycle regulation and cancer progression. Its selective inhibition of CDKs allows researchers to investigate the underlying mechanisms of action and potential therapeutic benefits in preclinical models.
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.
Check Digit Verification of cas no
The CAS Registry Mumber 345627-80-7 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,4,5,6,2 and 7 respectively; the second part has 2 digits, 8 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 345627-80:
(8*3)+(7*4)+(6*5)+(5*6)+(4*2)+(3*7)+(2*8)+(1*0)=157
157 % 10 = 7
So 345627-80-7 is a valid CAS Registry Number.
InChI:InChI=1/C17H24N4O2S2/c1-17(2,3)12-8-19-13(23-12)10-24-14-9-20-16(25-14)21-15(22)11-4-6-18-7-5-11/h8-9,11,18H,4-7,10H2,1-3H3,(H,20,21,22)
345627-80-7Relevant academic research and scientific papers
CDK INHIBITORS CONTAINING A ZINC BINDING MOIETY
-
, (2009/04/25)
The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.
N-(Cycloalkylamino)acyl-2-aminothiazole Inhibitors of Cyclin-Dependent Kinase 2. N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl] -4-piperidinecarboxamide (BMS-387032), a Highly Efficacious and Selective Antitumor Agent
Misra, Raj N.,Xiao, Hai-Yun,Kim, Kyoung S.,Lu, Songfeng,Han, Wen-Ching,Barbosa, Stephanie A.,Hunt, John T.,Rawlins, David B.,Shan, Weifang,Ahmed, Syed Z.,Qian, Ligang,Chen, Bang-Chi,Zhao, Rulin,Bednarz, Mark S.,Kellar, Kristen A.,Mulheron, Janet G.,Batorsky, Roberta,Roongta, Urvashi,Kamath, Amrita,Marathe, Punit,Ranadive, Sunanda A.,Sack, John S.,Tokarski, John S.,Pavletich, Nikola P.,Lee, Francis Y. F.,Webster, Kevin R.,Kimball, S. David
, p. 1719 - 1728 (2007/10/03)
N-Acyl-2-aminothiazoles with nonaromatic acyl side chains containing a basic amine were found to be potent, selective inhibitors of CDK2/cycE which exhibit antitumor activity in mice. In particular, compound 21 {N-[5-[[[5-(1,1-dimethylethyl)-2- oxazolyl]m
