KW-2450 Tosylate salt

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

MedKoo CAT#: 205908

CAS#: 1360433-93-7 (tosylate)

Description: KW-2450 is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.


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10mg
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100mg
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1g
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25mg
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200mg
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2g
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50mg
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500mg
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5g
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KW-2450 Tosylate salt is not in stock, but may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205908
Name: KW-2450 Tosylate salt
CAS#: 1360433-93-7 (tosylate)
Chemical Formula: C35H37N5O6S2
Exact Mass: 687.2185
Molecular Weight: 687.83
Elemental Analysis: C, 61.12; H, 5.42; N, 10.18; O, 13.96; S, 9.32


Related CAS #: 1360433-93-7 (tosylate)   904899-25-8 (free base)  

Synonym: KW2450; KW-2450; KW 2450.

IUPAC/Chemical Name: (E)-N-(2-(2-(1H-indazol-3-yl)vinyl)-5-((4-(2-hydroxyacetyl)piperazin-1-yl)methyl)phenyl)-3-methylthiophene-2-carboxamide 4-methylbenzenesulfonate

InChi Key: SIJKXSMUXNJNQM-HRNDJLQDSA-N

InChi Code: InChI=1S/C28H29N5O3S.C7H8O3S/c1-19-10-15-37-27(19)28(36)29-25-16-20(17-32-11-13-33(14-12-32)26(35)18-34)6-7-21(25)8-9-24-22-4-2-3-5-23(22)30-31-24;1-6-2-4-7(5-3-6)11(8,9)10/h2-10,15-16,34H,11-14,17-18H2,1H3,(H,29,36)(H,30,31);2-5H,1H3,(H,8,9,10)/b9-8+;

SMILES Code: O=C(C1=C(C)C=CS1)NC2=CC(CN3CCN(C(CO)=O)CC3)=CC=C2/C=C/C4=NNC5=C4C=CC=C5.OS(=O)(C6=CC=C(C)C=C6)=O


Technical Data

Appearance:
Solid powder

Purity:
>98%

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:
>5 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).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

 1: Schwartz G, Dickson M, LoRusso P, Sausville E, Maekawa Y, Watanabe Y, Kashima N, Nakashima D, Akinaga S. Pre-clinical and first-in-human phase I studies of KW-2450, an oral tyrosine kinase inhibitor with IGF-1R/IR selectivity. Cancer Sci. 2016 Feb 6. doi: 10.1111/cas.12906. [Epub ahead of print] PubMed PMID: 26850678.

2: Kai K, Kondo K, Wang X, Xie X, Pitner MK, Reyes ME, Torres-Adorno AM, Masuda H, Hortobagyi GN, Bartholomeusz C, Saya H, Tripathy D, Sen S, Ueno NT. Antitumor Activity of KW-2450 against Triple-Negative Breast Cancer by Inhibiting Aurora A and B Kinases. Mol Cancer Ther. 2015 Dec;14(12):2687-99. doi: 10.1158/1535-7163.MCT-15-0096. Epub 2015 Oct 6. PubMed PMID: 26443806; PubMed Central PMCID: PMC4674309.

3: Williams R. Discontinued in 2013: oncology drugs. Expert Opin Investig Drugs. 2015 Jan;24(1):95-110. Epub 2014 Oct 14. PubMed PMID: 25315907.

4: Balasubramanian S, Allen JD, Kanitkar A, Boldor D. Oil extraction from Scenedesmus obliquus using a continuous microwave system--design, optimization, and quality characterization. Bioresour Technol. 2011 Feb;102(3):3396-403. doi: 10.1016/j.biortech.2010.09.119. Epub 2010 Oct 8. PubMed PMID: 20980140.

5: Reddy TS, Bazan NG. Arachidonic acid, stearic acid, and diacylglycerol accumulation correlates with the loss of phosphatidylinositol 4,5-bisphosphate in cerebrum 2 seconds after electroconvulsive shock: complete reversion of changes 5 minutes after stimulation. J Neurosci Res. 1987;18(3):449-55. PubMed PMID: 2830409.

6: Miller AL. Regional glucose and beta-hydroxybutyrate use by developing rat brain. Metab Brain Dis. 1986 Mar;1(1):53-61. PubMed PMID: 3508236.

7: Ikarashi Y, Sasahara T, Maruyama Y. [A simple method for determination of choline (Ch) and acetylcholine (ACh) in rat brain regions using high-performance liquid chromatography with electrochemical detection (HPLC-ED)]. Nihon Yakurigaku Zasshi. 1984 Dec;84(6):529-36. Japanese. PubMed PMID: 6549170.