KW-2450 Tosylate

    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.


Chemical Structure

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KW-2450 Tosylate
CAS# 1360433-93-7 (tosylate)

Theoretical Analysis

MedKoo Cat#: 205908
Name: KW-2450 Tosylate
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

Size Price Shipping out time Quantity
Inquire bulk and customized quantity

Pricing updated 2021-03-01. Prices are subject to change without notice.

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.

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

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).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 687.83 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Umehara H, Maekawa Y, Koizumi F, Shimizu M, Ota T, Fouad TM, Willey J, Kaito H, Shiraishi N, Nakashima D, Akinaga S, Ueno NT. Preclinical and phase I clinical studies of KW-2450, a dual IGF-1R/IR tyrosine kinase inhibitor, in combination with lapatinib and letrozole. Ther Adv Med Oncol. 2018 Jul 30;10:1758835918786858. doi: 10.1177/1758835918786858. PMID: 30083253; PMCID: PMC6066809.

2: Schwartz GK, Dickson MA, LoRusso PM, Sausville EA, Maekawa Y, Watanabe Y, Kashima N, Nakashima D, Akinaga S. Preclinical and first-in-human phase I studies of KW-2450, an oral tyrosine kinase inhibitor with insulin-like growth factor receptor-1/insulin receptor selectivity. Cancer Sci. 2016 Apr;107(4):499-506. doi: 10.1111/cas.12906. Epub 2016 Mar 28. PMID: 26850678; PMCID: PMC4832855.

3: 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. PMID: 26443806; PMCID: PMC4674309.

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7: Miller AL. Regional glucose and beta-hydroxybutyrate use by developing rat brain. Metab Brain Dis. 1986 Mar;1(1):53-61. doi: 10.1007/BF00998477. PMID: 3508236.

8: 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. doi: 10.1254/fpj.84.529. PMID: 6549170.



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