SNS-314 free base | 1057249-41-8 | 1146618-41-8 | AK inhibitor

MedKoo Cat#: 202651 | Name: SNS-314

Description:

WARNING: This product is for research use only, not for human or veterinary use.

SNS-314 is a synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity. Aurora kinase inhibitor SNS-314 selectively binds to and inhibits AKs A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress AKs. AKs are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis.

Chemical Structure

SNS-314

CAS#1057249-41-8 (free base)

Theoretical Analysis

MedKoo Cat#: 202651

Name: SNS-314

CAS#: 1057249-41-8 (free base)

Chemical Formula: C18H15ClN6OS2

Exact Mass: 430.0437

Molecular Weight: 430.93

Elemental Analysis: C, 50.17; H, 3.51; Cl, 8.23; N, 19.50; O, 3.71; S, 14.88.

Price and Availability

Size	Price	Availability
5mg	USD 90.00	Ready to ship
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship
200mg	USD 1,250.00	Ready to ship
500mg	USD 2,850.00	Ready to ship

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Related CAS #

1057249-41-8 (free base) 1146618-41-8 (mesylate)

Synonym

SNS314; SNS-314; SNS 314; SNS-314 free base;

IUPAC/Chemical Name

N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea.

InChi Key

FAYAUAZLLLJJGH-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H15ClN6OS2/c19-11-2-1-3-12(8-11)24-17(26)25-18-21-9-13(28-18)4-6-20-16-15-14(5-7-27-15)22-10-23-16/h1-3,5,7-10H,4,6H2,(H,20,22,23)(H2,21,24,25,26)

SMILES Code

O=C(NC1=NC=C(CCNC2=C3C(C=CS3)=NC=N2)S1)NC4=CC=CC(Cl)=C4

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

Related CAS# 1057249-41-8 ( SNS-314 free base) 1146618-41-8 ( SNS-314 mesylate).

Product Data

Product Data

Certificate of Analysis

View current batch of CoA, Lot#BBC31209

QC Data

View QC data: current batch, Lot#BBC31209

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

SNS-314 is an aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively.

In vitro activity:

This study demonstrates that SNS-314 is a potential therapeutic agent in hepatocellular carcinoma (HCC), potentially in combination with Hippo pathway inhibitors. SNS-314, more effective than selective inhibitors, induced apoptosis and polyploidy in HCC by suppressing YAP and increasing P21. P21 enhanced the apoptotic effect of SNS-314 in HCC. Reference: Oncotarget. 2017 Apr 25;8(17):27953-27965. https://pubmed.ncbi.nlm.nih.gov/28427193/

In vivo activity:

SNS-314 has been developed as a novel anti-cancer therapeutic agent for the treatment of diverse human malignancies. In a human colon cancer xenograft model, SNS-314 treatment led to dose-dependent inhibition of histone H3 phosphorylation. After SNS-314, HCT116 tumors showed potent and sustained responses, including reduced phosphorylated histone H3 levels, increased caspase-3, and appearance of increased nuclear size. Reference: Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17. https://pubmed.ncbi.nlm.nih.gov/19649632/

	Solvent	mg/mL	mM
Solubility
	DMSO	100.9	234.14

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 430.93 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.

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. Liu F, Wang G, Wang X, Che Z, Dong W, Guo X, Wang Z, Chen P, Hou D, Zhang Q, Zhang W, Pan Y, Yang D, Liu H. Targeting high Aurora kinases expression as an innovative therapy for hepatocellular carcinoma. Oncotarget. 2017 Apr 25;8(17):27953-27965. doi: 10.18632/oncotarget.15853. PMID: 28427193; PMCID: PMC5438621. 2. Baldini E, Sorrenti S, D'Armiento E, Guaitoli E, Morrone S, D'Andrea V, Gnessi L, Moretti C, Antonelli A, Catania A, De Antoni E, Ulisse S. Effects of the Aurora kinases pan-inhibitor SNS-314 mesylate on anaplastic thyroid cancer derived cell lines. Clin Ter. 2012;163(5):e307-13. PMID: 23099978. 3. Arbitrario JP, Belmont BJ, Evanchik MJ, Flanagan WM, Fucini RV, Hansen SK, Harris SO, Hashash A, Hoch U, Hogan JN, Howlett AR, Jacobs JW, Lam JW, Ritchie SC, Romanowski MJ, Silverman JA, Stockett DE, Teague JN, Zimmerman KM, Taverna P. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17. doi: 10.1007/s00280-009-1076-8. Epub 2009 Aug 1. PMID: 19649632. 4. VanderPorten EC, Taverna P, Hogan JN, Ballinger MD, Flanagan WM, Fucini RV. The Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model. Mol Cancer Ther. 2009 Apr;8(4):930-9. doi: 10.1158/1535-7163.MCT-08-0754. PMID: 19372566.

In vitro protocol:

In vivo protocol:

1. Arbitrario JP, Belmont BJ, Evanchik MJ, Flanagan WM, Fucini RV, Hansen SK, Harris SO, Hashash A, Hoch U, Hogan JN, Howlett AR, Jacobs JW, Lam JW, Ritchie SC, Romanowski MJ, Silverman JA, Stockett DE, Teague JN, Zimmerman KM, Taverna P. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17. doi: 10.1007/s00280-009-1076-8. Epub 2009 Aug 1. PMID: 19649632. 2. VanderPorten EC, Taverna P, Hogan JN, Ballinger MD, Flanagan WM, Fucini RV. The Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model. Mol Cancer Ther. 2009 Apr;8(4):930-9. doi: 10.1158/1535-7163.MCT-08-0754. PMID: 19372566.

1: Liu F, Wang G, Wang X, Che Z, Dong W, Guo X, Wang Z, Chen P, Hou D, Zhang Q, Zhang W, Pan Y, Yang D, Liu H. Targeting high Aurora kinases expression as an innovative therapy for hepatocellular carcinoma. Oncotarget. 2017 Apr 25;8(17):27953-27965. doi: 10.18632/oncotarget.15853. PubMed PMID: 28427193; PubMed Central PMCID: PMC5438621. 2: Quagliariello V, Armenia E, Aurilio C, Rosso F, Clemente O, de Sena G, Barbarisi M, Barbarisi A. New Treatment of Medullary and Papillary Human Thyroid Cancer: Biological Effects of Hyaluronic Acid Hydrogel Loaded With Quercetin Alone or in Combination to an Inhibitor of Aurora Kinase. J Cell Physiol. 2016 Aug;231(8):1784-95. doi: 10.1002/jcp.25283. Epub 2016 Feb 2. PubMed PMID: 26660542. 3: Sarvagalla S, Coumar MS. Structural Biology Insight for the Design of Sub-type Selective Aurora Kinase Inhibitors. Curr Cancer Drug Targets. 2015;15(5):375-93. Review. PubMed PMID: 25895501. 4: Cheung CH, Sarvagalla S, Lee JY, Huang YC, Coumar MS. Aurora kinase inhibitor patents and agents in clinical testing: an update (2011 - 2013). Expert Opin Ther Pat. 2014 Sep;24(9):1021-38. doi: 10.1517/13543776.2014.931374. Epub 2014 Jun 26. Review. PubMed PMID: 24965505. 5: Baldini E, Sorrenti S, D'Armiento E, Guaitoli E, Morrone S, D'Andrea V, Gnessi L, Moretti C, Antonelli A, Catania A, De Antoni E, Ulisse S. Effects of the Aurora kinases pan-inhibitor SNS-314 mesylate on anaplastic thyroid cancer derived cell lines. Clin Ter. 2012;163(5):e307-13. PubMed PMID: 23099978. 6: Zhang B, Li Y, Zhang H, Ai C. 3D-QSAR and molecular docking studies on derivatives of MK-0457, GSK1070916 and SNS-314 as inhibitors against Aurora B kinase. Int J Mol Sci. 2010 Nov 2;11(11):4326-47. doi: 10.3390/ijms11114326. PubMed PMID: 21151441; PubMed Central PMCID: PMC3000085. 7: Lok W, Klein RQ, Saif MW. Aurora kinase inhibitors as anti-cancer therapy. Anticancer Drugs. 2010 Apr;21(4):339-50. doi: 10.1097/CAD.0b013e3283350dd1. Review. PubMed PMID: 20016367. 8: Arbitrario JP, Belmont BJ, Evanchik MJ, Flanagan WM, Fucini RV, Hansen SK, Harris SO, Hashash A, Hoch U, Hogan JN, Howlett AR, Jacobs JW, Lam JW, Ritchie SC, Romanowski MJ, Silverman JA, Stockett DE, Teague JN, Zimmerman KM, Taverna P. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17. doi: 10.1007/s00280-009-1076-8. Epub 2009 Aug 1. PubMed PMID: 19649632. 9: Zhong M, Bui M, Shen W, Baskaran S, Allen DA, Elling RA, Flanagan WM, Fung AD, Hanan EJ, Harris SO, Heumann SA, Hoch U, Ivy SN, Jacobs JW, Lam S, Lee H, McDowell RS, Oslob JD, Purkey HE, Romanowski MJ, Silverman JA, Tangonan BT, Taverna P, Yang W, Yoburn JC, Yu CH, Zimmerman KM, O'Brien T, Lew W. 2-Aminobenzimidazoles as potent Aurora kinase inhibitors. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5158-61. doi: 10.1016/j.bmcl.2009.07.016. Epub 2009 Jul 9. PubMed PMID: 19646866. 10: VanderPorten EC, Taverna P, Hogan JN, Ballinger MD, Flanagan WM, Fucini RV. The Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model. Mol Cancer Ther. 2009 Apr;8(4):930-9. doi: 10.1158/1535-7163.MCT-08-0754. PubMed PMID: 19372566. 11: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2009 Jan-Feb;31(1):47-57. PubMed PMID: 19357798. 12: Oslob JD, Heumann SA, Yu CH, Allen DA, Baskaran S, Bui M, Delarosa E, Fung AD, Hashash A, Hau J, Ivy S, Jacobs JW, Lew W, Maung J, McDowell RS, Ritchie S, Romanowski MJ, Silverman JA, Yang W, Zhong M, Fuchs-Knotts T. Water-soluble prodrugs of an Aurora kinase inhibitor. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1409-12. doi: 10.1016/j.bmcl.2009.01.043. Epub 2009 Jan 19. PubMed PMID: 19186057. 13: Oslob JD, Romanowski MJ, Allen DA, Baskaran S, Bui M, Elling RA, Flanagan WM, Fung AD, Hanan EJ, Harris S, Heumann SA, Hoch U, Jacobs JW, Lam J, Lawrence CE, McDowell RS, Nannini MA, Shen W, Silverman JA, Sopko MM, Tangonan BT, Teague J, Yoburn JC, Yu CH, Zhong M, Zimmerman KM, O'Brien T, Lew W. Discovery of a potent and selective aurora kinase inhibitor. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4880-4. doi: 10.1016/j.bmcl.2008.07.073. Epub 2008 Jul 24. PubMed PMID: 18678489.