KW-2450 Tosylate

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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

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: 687.22
Molecular Weight: 687.830
Elemental Analysis: C, 61.12; H, 5.42; N, 10.18; O, 13.96; S, 9.32

Price and Availability

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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 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+;


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

More Info:         

Biological target:
In vitro activity:
In vivo activity:

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.

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:
In vitro protocol:
In vivo protocol:

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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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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.