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MedKoo Cat#: 462478 | Name: SCH-1473759 HCl
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Description:

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

SCH-1473759 is a potent and selective Aurora A/B inhibitor with IC50 sub-nanomolar. SCH 1473759 was active against a large panel of tumor cell lines from different tissue origin and genetic backgrounds. SCH-1473759 demonstrated potent mechanism-based activity, and activity was shown to be enhanced in combination with taxanes and KSP inhibitors. This information may be useful for optimizing the clinical efficacy of Aurora inhibitors.

Chemical Structure

SCH-1473759 HCl
SCH-1473759 HCl
CAS#1094067-13-6 (HCl)

Theoretical Analysis

MedKoo Cat#: 462478

Name: SCH-1473759 HCl

CAS#: 1094067-13-6 (HCl)

Chemical Formula: C20H27ClN8OS

Exact Mass: 0.0000

Molecular Weight: 463.00

Elemental Analysis: C, 51.88; H, 5.88; Cl, 7.66; N, 24.20; O, 3.46; S, 6.92

Price and Availability

Size Price Availability Quantity
2mg USD 350.00 2 Weeks
5mg USD 750.00 2 Weeks
10mg USD 1,250.00 2 Weeks
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Related CAS #
1094069-99-4 (free base) 1094067-13-6 (HCl)
Synonym
SCH-1473759 hydrochloride; SCH1473759; SCH-1473759 ; SCH 1473759;
IUPAC/Chemical Name
2-(ethyl((5-((6-methyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)amino)isothiazol-3-yl)methyl)amino)-2-methylpropan-1-ol hydrochloride
InChi Key
YBAZMWNWFHDNTH-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H26N8OS.ClH/c1-5-27(20(3,4)12-29)11-15-6-17(30-26-15)25-18-19-21-9-16(14-7-22-23-8-14)28(19)10-13(2)24-18;/h6-10,29H,5,11-12H2,1-4H3,(H,22,23)(H,24,25);1H
SMILES Code
[H]Cl.CC1=CN2C(C(NC3=CC(CN(C(C)(CO)C)CC)=NS3)=N1)=NC=C2C4=CNN=C4
Appearance
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 and water
Shelf Life
>3 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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SCH-1473759 HCl is an aurora inhibitor with IC50s of 4 and 13 nM for aurora A and B, respectively.
In vitro activity:
This study investigated SCH-1473759’s effects across a large panel of tumor cell lines from different tissue origin and genetic backgrounds. SCH-1473759 caused DNA content changes and inhibited cell growth after different exposure times. SCH 1473759 accelerated cell exit from mitosis following arrest induced by taxanes or KSP inhibitors. Reference: Cancer Chemother Pharmacol. 2011 Oct;68(4):923-33. https://pubmed.ncbi.nlm.nih.gov/21298383/
In vivo activity:
In this study, a novel UHPLC-MS/MS method was established to measure SCH-1473759 in murine plasma. There was a maximum plasma concentration of 34ng/mL at 1h, a half-life of 1h, and poor oral bioavailability (F=0.002). Reference: J Pharm Biomed Anal. 2017 Jan 5;132:223-226. https://pubmed.ncbi.nlm.nih.gov/27768921/
Solvent mg/mL mM
Solubility
DMSO 7.1 15.42
Water 8.3 17.99
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 463.00 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. Basso AD, Liu M, Gray K, Tevar S, Lee S, Liang L, Ponery A, Smith EB, Monsma FJ Jr, Yu T, Zhang Y, Kerekes AD, Esposite S, Xiao Y, Tagat JR, Hicklin DJ, Kirschmeier P. SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors. Cancer Chemother Pharmacol. 2011 Oct;68(4):923-33. doi: 10.1007/s00280-011-1568-1. Epub 2011 Feb 5. PMID: 21298383. 2. Yu T, Tagat JR, Kerekes AD, Doll RJ, Zhang Y, Xiao Y, Esposite S, Belanger DB, Curran PJ, Mandal AK, Siddiqui MA, Shih NY, Basso AD, Liu M, Gray K, Tevar S, Jones J, Lee S, Liang L, Ponery S, Smith EB, Hruza A, Voigt J, Ramanathan L, Prosise W, Hu M. Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core. ACS Med Chem Lett. 2010 Jun 7;1(5):214-8. doi: 10.1021/ml100063w. PMID: 24900197; PMCID: PMC4007894. 3. Ferraz Nogueira Filho MA, Peer CJ, Nguyen J, McCalla A, Helman L, Figg WD. A simple and rapid UHPLC-MS/MS method for the quantitation of the dual aurora kinase A/B inhibitor SCH-1473759 in murine plasma. J Pharm Biomed Anal. 2017 Jan 5;132:223-226. doi: 10.1016/j.jpba.2016.10.003. Epub 2016 Oct 5. PMID: 27768921; PMCID: PMC6357958.
In vitro protocol:
1. Basso AD, Liu M, Gray K, Tevar S, Lee S, Liang L, Ponery A, Smith EB, Monsma FJ Jr, Yu T, Zhang Y, Kerekes AD, Esposite S, Xiao Y, Tagat JR, Hicklin DJ, Kirschmeier P. SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors. Cancer Chemother Pharmacol. 2011 Oct;68(4):923-33. doi: 10.1007/s00280-011-1568-1. Epub 2011 Feb 5. PMID: 21298383. 2. Yu T, Tagat JR, Kerekes AD, Doll RJ, Zhang Y, Xiao Y, Esposite S, Belanger DB, Curran PJ, Mandal AK, Siddiqui MA, Shih NY, Basso AD, Liu M, Gray K, Tevar S, Jones J, Lee S, Liang L, Ponery S, Smith EB, Hruza A, Voigt J, Ramanathan L, Prosise W, Hu M. Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core. ACS Med Chem Lett. 2010 Jun 7;1(5):214-8. doi: 10.1021/ml100063w. PMID: 24900197; PMCID: PMC4007894.
In vivo protocol:
1. Ferraz Nogueira Filho MA, Peer CJ, Nguyen J, McCalla A, Helman L, Figg WD. A simple and rapid UHPLC-MS/MS method for the quantitation of the dual aurora kinase A/B inhibitor SCH-1473759 in murine plasma. J Pharm Biomed Anal. 2017 Jan 5;132:223-226. doi: 10.1016/j.jpba.2016.10.003. Epub 2016 Oct 5. PMID: 27768921; PMCID: PMC6357958.
1: Yu T, Tagat JR, Kerekes AD, et al. Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core. ACS Med Chem Lett. 2010;1(5):214-218. Published 2010 Jun 7. doi:10.1021/ml100063w 2: Basso AD, Liu M, Gray K, et al. SCH 1473759, a novel Aurora inhibitor, demonstrates enhanced anti-tumor activity in combination with taxanes and KSP inhibitors. Cancer Chemother Pharmacol. 2011;68(4):923-933. doi:10.1007/s00280-011-1568-1

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