SNS-032
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MedKoo CAT#: 202640

CAS#: 345627-80-7 (free base)

Description: SNS-032, also known as BMS-387032, is a 2-aminothiazole-derived, small-molecule cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. CDK inhibitor SNS-032 selectively binds to CDKs 2, 7, and 9, preventing their phosphorylation and activation; inhibition of CDK activity may result in cell cycle arrest, the induction of apoptosis and decreased tumor cell proliferation in susceptible tumor cell populations. This agent has been shown to sensitize radioresistant tumor cells to ionizing radiation.

Chemical Structure

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SNS-032
CAS# 345627-80-7 (free base)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 202640
Name: SNS-032
CAS#: 345627-80-7 (free base)
Chemical Formula: C17H24N4O2S2
Exact Mass: 380.13
Molecular Weight: 380.530
Elemental Analysis: C, 53.66; H, 6.36; N, 14.72; O, 8.41; S, 16.85

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 400 Ready to ship
100mg USD 650 Ready to ship
200mg USD 1150 Ready to ship
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Related CAS #: 345627-80-7 (free base)   345627-90-9 (HCl),  

Synonym: SNS 032; SNS032; SNS-032; BMS387032; BMS 387032; BMS-387032

IUPAC/Chemical Name: N-(5-(((5-(1,1-dimethylethyl)-2-oxazolyl)methyl)thio)-2-thiazolyl)-4-piperidinecarboxamide

InChi Key: OUSFTKFNBAZUKL-UHFFFAOYSA-N

InChi Code: InChI=1S/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)

SMILES Code: O=C(C1CCNCC1)NC2=NC=C(SCC3=NC=C(C(C)(C)C)O3)S2

Appearance: white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: SNS-032 selectively inhibits CDK2, CDK7, and CDK9. CDK2 and CDK7 are active in cell-cycle progression. CDK7 is also active in promoting transcription, as is CDK9. SNS-032 therefore has dual mechanisms of action-inhibiting proliferation by blocking replication, and inducing apoptosis by blocking transcription to turn off survival and growth factors. (from: http://sunesis.com/science/oncology/MOA032.php).    

Biological target: SNS-032 is a potent and selective inhibitor of CDK2, CDK7, and CDK9 with IC50s of 38 nM, 62 nM and 4 nM, respectively.
In vitro activity: This study indicates that SNS-032 is a promising therapeutic agent for esophageal squamous cell carcinoma treatment. SNS-032 effectively inhibited cellular viability, abrogated anchorage-independent growth, and potentiated the sensitivity to cisplatin in ESCC cells. SNS-032 induced a mitochondrial-dependent apoptosis of ESCC cells by reducing Mcl-1 transcription and potently abrogated the abilities of ESCC cell migration and invasion through transcriptional downregulation of MMP-1. Reference: Cell Death Dis. 2021 Nov 5;12(11):1048. https://pubmed.ncbi.nlm.nih.gov/34741018/
In vivo activity: SNS-032 is a potential drug and CDK9 might be a new prospective target for the treatment of liver fibrosis. In a mouse model of liver fibrosis, SNS-032 was found to alleviate hepatic fibrosis by inhibiting the activation and inducing the apoptosis of active hepatic stellate cells. Reference: Front Pharmacol. 2022 Oct 12;13:1016552. https://pubmed.ncbi.nlm.nih.gov/36313366/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 42.8 112.47

Preparing Stock Solutions

The following data is based on the product molecular weight 380.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Zeng H, Yang H, Song Y, Fang D, Chen L, Zhao Z, Wang C, Xie S. Transcriptional inhibition by CDK7/9 inhibitor SNS-032 suppresses tumor growth and metastasis in esophageal squamous cell carcinoma. Cell Death Dis. 2021 Nov 5;12(11):1048. doi: 10.1038/s41419-021-04344-w. PMID: 34741018; PMCID: PMC8571299. 2. Meng H, Jin Y, Liu H, You L, Yang C, Yang X, Qian W. SNS-032 inhibits mTORC1/mTORC2 activity in acute myeloid leukemia cells and has synergistic activity with perifosine against Akt. J Hematol Oncol. 2013 Feb 18;6:18. doi: 10.1186/1756-8722-6-18. PMID: 23415012; PMCID: PMC3599109. 3. He XL, Hu YH, Chen JM, Zhang DQ, Yang HL, Zhang LZ, Mu YP, Zhang H, Chen GF, Liu W, Liu P. SNS-032 attenuates liver fibrosis by anti-active hepatic stellate cells via inhibition of cyclin dependent kinase 9. Front Pharmacol. 2022 Oct 12;13:1016552. doi: 10.3389/fphar.2022.1016552. PMID: 36313366; PMCID: PMC9597511. 4. Jiang L, Wen C, Zhou H, Liu A, Zhang H, Chen X, Ding W, Liu J, Shi X. Cyclin-dependent kinase 7/9 inhibitor SNS-032 induces apoptosis in diffuse large B-cell lymphoma cells. Cancer Biol Ther. 2022 Dec 31;23(1):319-327. doi: 10.1080/15384047.2022.2055421. PMID: 35332847; PMCID: PMC8959513.
In vitro protocol: 1. Zeng H, Yang H, Song Y, Fang D, Chen L, Zhao Z, Wang C, Xie S. Transcriptional inhibition by CDK7/9 inhibitor SNS-032 suppresses tumor growth and metastasis in esophageal squamous cell carcinoma. Cell Death Dis. 2021 Nov 5;12(11):1048. doi: 10.1038/s41419-021-04344-w. PMID: 34741018; PMCID: PMC8571299. 2. Meng H, Jin Y, Liu H, You L, Yang C, Yang X, Qian W. SNS-032 inhibits mTORC1/mTORC2 activity in acute myeloid leukemia cells and has synergistic activity with perifosine against Akt. J Hematol Oncol. 2013 Feb 18;6:18. doi: 10.1186/1756-8722-6-18. PMID: 23415012; PMCID: PMC3599109.
In vivo protocol: 1. He XL, Hu YH, Chen JM, Zhang DQ, Yang HL, Zhang LZ, Mu YP, Zhang H, Chen GF, Liu W, Liu P. SNS-032 attenuates liver fibrosis by anti-active hepatic stellate cells via inhibition of cyclin dependent kinase 9. Front Pharmacol. 2022 Oct 12;13:1016552. doi: 10.3389/fphar.2022.1016552. PMID: 36313366; PMCID: PMC9597511. 2. Jiang L, Wen C, Zhou H, Liu A, Zhang H, Chen X, Ding W, Liu J, Shi X. Cyclin-dependent kinase 7/9 inhibitor SNS-032 induces apoptosis in diffuse large B-cell lymphoma cells. Cancer Biol Ther. 2022 Dec 31;23(1):319-327. doi: 10.1080/15384047.2022.2055421. PMID: 35332847; PMCID: PMC8959513.

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1: Xie G, Tang H, Wu S, Chen J, Liu J, Liao C. The cyclin-dependent kinase inhibitor SNS-032 induces apoptosis in breast cancer cells via depletion of Mcl-1 and X-linked inhibitor of apoptosis protein and displays antitumor activity in vivo. Int J Oncol. 2014 Aug;45(2):804-12. doi: 10.3892/ijo.2014.2467. Epub 2014 May 26. PubMed PMID: 24865236.

2: Löschmann N, Michaelis M, Rothweiler F, Zehner R, Cinatl J, Voges Y, Sharifi M, Riecken K, Meyer J, von Deimling A, Fichtner I, Ghafourian T, Westermann F, Cinatl J Jr. Testing of SNS-032 in a Panel of Human Neuroblastoma Cell Lines with Acquired Resistance to a Broad Range of Drugs. Transl Oncol. 2013 Dec 1;6(6):685-96. eCollection 2013 Dec 1. PubMed PMID: 24466371; PubMed Central PMCID: PMC3890703.

3: Cihalova D, Hofman J, Ceckova M, Staud F. Purvalanol A, olomoucine II and roscovitine inhibit ABCB1 transporter and synergistically potentiate cytotoxic effects of daunorubicin in vitro. PLoS One. 2013 Dec 23;8(12):e83467. doi: 10.1371/journal.pone.0083467. eCollection 2013. PubMed PMID: 24376706; PubMed Central PMCID: PMC3871618.

4: Lemke J, von Karstedt S, Abd El Hay M, Conti A, Arce F, Montinaro A, Papenfuss K, El-Bahrawy MA, Walczak H. Selective CDK9 inhibition overcomes TRAIL resistance by concomitant suppression of cFlip and Mcl-1. Cell Death Differ. 2014 Mar;21(3):491-502. doi: 10.1038/cdd.2013.179. Epub 2013 Dec 20. PubMed PMID: 24362439; PubMed Central PMCID: PMC3921597.

5: Qi RZ, Ji Q, Zhang LY, Zhang Y, Yuan WP, Cheng T, Gao YD, Xu J. [Effect of SNS-032 on biological activity of hematopoietic stem cells in mice]. Zhongguo Shi Yan Xue Ye Xue Za Zhi. 2013 Jun;21(3):741-5. doi: 10.7534/j.issn.1009-2137.2013.03.040. Chinese. PubMed PMID: 23815933.

6: Meng H, Jin Y, Liu H, You L, Yang C, Yang X, Qian W. SNS-032 inhibits mTORC1/mTORC2 activity in acute myeloid leukemia cells and has synergistic activity with perifosine against Akt. J Hematol Oncol. 2013 Feb 18;6:18. doi: 10.1186/1756-8722-6-18. PubMed PMID: 23415012; PubMed Central PMCID: PMC3599109.

7: Gallorini M, Cataldi A, di Giacomo V. Cyclin-dependent kinase modulators and cancer therapy. BioDrugs. 2012 Dec 1;26(6):377-91. doi: 10.2165/11634060-000000000-00000. Review. PubMed PMID: 22928661.

8: Robak P, Robak T. A targeted therapy for protein and lipid kinases in chronic lymphocytic leukemia. Curr Med Chem. 2012;19(31):5294-318. Review. PubMed PMID: 22830347.

9: Held JM, Britton DJ, Scott GK, Lee EL, Schilling B, Baldwin MA, Gibson BW, Benz CC. Ligand binding promotes CDK-dependent phosphorylation of ER-alpha on hinge serine 294 but inhibits ligand-independent phosphorylation of serine 305. Mol Cancer Res. 2012 Aug;10(8):1120-32. doi: 10.1158/1541-7786.MCR-12-0099. Epub 2012 Jun 5. PubMed PMID: 22669764; PubMed Central PMCID: PMC3950940.

10: Wu Y, Chen C, Sun X, Shi X, Jin B, Ding K, Yeung SC, Pan J. Cyclin-dependent kinase 7/9 inhibitor SNS-032 abrogates FIP1-like-1 platelet-derived growth factor receptor α and bcr-abl oncogene addiction in malignant hematologic cells. Clin Cancer Res. 2012 Apr 1;18(7):1966-78. doi: 10.1158/1078-0432.CCR-11-1971. Epub 2012 Mar 23. PubMed PMID: 22447844.

11: Walsby E, Lazenby M, Pepper C, Burnett AK. The cyclin-dependent kinase inhibitor SNS-032 has single agent activity in AML cells and is highly synergistic with cytarabine. Leukemia. 2011 Mar;25(3):411-9. doi: 10.1038/leu.2010.290. Epub 2011 Jan 7. PubMed PMID: 21212792.

12: Chen R, Guo L, Chen Y, Jiang Y, Wierda WG, Plunkett W. Homoharringtonine reduced Mcl-1 expression and induced apoptosis in chronic lymphocytic leukemia. Blood. 2011 Jan 6;117(1):156-64. doi: 10.1182/blood-2010-01-262808. Epub 2010 Oct 22. PubMed PMID: 20971952; PubMed Central PMCID: PMC3037741.

13: Kruse U, Pallasch CP, Bantscheff M, Eberhard D, Frenzel L, Ghidelli S, Maier SK, Werner T, Wendtner CM, Drewes G. Chemoproteomics-based kinome profiling and target deconvolution of clinical multi-kinase inhibitors in primary chronic lymphocytic leukemia cells. Leukemia. 2011 Jan;25(1):89-100. doi: 10.1038/leu.2010.233. Epub 2010 Oct 14. PubMed PMID: 20944678.

14: Chen R, Chubb S, Cheng T, Hawtin RE, Gandhi V, Plunkett W. Responses in mantle cell lymphoma cells to SNS-032 depend on the biological context of each cell line. Cancer Res. 2010 Aug 15;70(16):6587-97. doi: 10.1158/0008-5472.CAN-09-3578. Epub 2010 Jul 27. PubMed PMID: 20663900; PubMed Central PMCID: PMC2929954.

15: Tong WG, Chen R, Plunkett W, Siegel D, Sinha R, Harvey RD, Badros AZ, Popplewell L, Coutre S, Fox JA, Mahadocon K, Chen T, Kegley P, Hoch U, Wierda WG. 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. J Clin Oncol. 2010 Jun 20;28(18):3015-22. doi: 10.1200/JCO.2009.26.1347. Epub 2010 May 17. PubMed PMID: 20479412.

16: Boquoi A, Chen T, Enders GH. Chemoprevention of mouse intestinal tumorigenesis by the cyclin-dependent kinase inhibitor SNS-032. Cancer Prev Res (Phila). 2009 Sep;2(9):800-6. doi: 10.1158/1940-6207.CAPR-09-0053. Epub 2009 Sep 1. PubMed PMID: 19723896; PubMed Central PMCID: PMC2819381.

17: Dickson MA, Schwartz GK. Development of cell-cycle inhibitors for cancer therapy. Curr Oncol. 2009 Mar;16(2):36-43. PubMed PMID: 19370178; PubMed Central PMCID: PMC2669234.

18: Ali MA, Reis A, Ding LH, Story MD, Habib AA, Chattopadhyay A, Saha D. SNS-032 prevents hypoxia-mediated glioblastoma cell invasion by inhibiting hypoxia inducible factor-1alpha expression. Int J Oncol. 2009 Apr;34(4):1051-60. PubMed PMID: 19287962.

19: Chen R, Wierda WG, Chubb S, Hawtin RE, Fox JA, Keating MJ, Gandhi V, Plunkett W. Mechanism of action of SNS-032, a novel cyclin-dependent kinase inhibitor, in chronic lymphocytic leukemia. Blood. 2009 May 7;113(19):4637-45. doi: 10.1182/blood-2008-12-190256. Epub 2009 Feb 20. PubMed PMID: 19234140; PubMed Central PMCID: PMC2680368.

20: Kodym E, Kodym R, Reis AE, Habib AA, Story MD, Saha D. The small-molecule CDK inhibitor, SNS-032, enhances cellular radiosensitivity in quiescent and hypoxic non-small cell lung cancer cells. Lung Cancer. 2009 Oct;66(1):37-47. doi: 10.1016/j.lungcan.2008.12.026. Epub 2009 Feb 3. PubMed PMID: 19193471.