Delving into the Latest Updates on KST-016366 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

Mechanism

Bcr-Abl T315I inhibitors(BCR-ABL T315I mutation inhibitors), Tie-2 antagonists(TEK receptor tyrosine kinase antagonists), TrkA antagonists(Nerve growth factor receptor Trk-A antagonists)

Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication-

Originator Organization

KIST Corp. (South Korea)

Active Organization

KIST Corp. (South Korea)

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

AbstractHerein we report the discovery of compound 6 [KST016366; 4‐((2‐(3‐(4‐((4‐ethylpiperazin‐1‐yl)methyl)‐3‐(trifluoromethyl)phenyl)ureido)benzo[d]thiazol‐6‐yl)oxy)picolinamide] as a new potent multikinase inhibitor through minor structural modification of our previously reported RAF kinase inhibitor A. In vitro anticancer evaluation of 6 showed substantial broad‐spectrum antiproliferative activity against 60 human cancer cell lines. In particular, it showed GI50 values of 51.4 and 19 nm against leukemia K‐562 and colon carcinoma KM12 cell lines, respectively. Kinase screening of compound 6 revealed its nanomolar‐level inhibitory activity of certain oncogenic kinases implicated in both tumorigenesis and angiogenesis. Interestingly, 6 displays IC50 values of 0.82, 3.81, and 53 nm toward Tie2, TrkA, and ABL‐1 (wild‐type and T315I mutant) kinases, respectively. Moreover, 6 is orally bioavailable with a favorable in vivo pharmacokinetic profile. Compound 6 may serve as a promising candidate for further development of potent anticancer chemotherapeutics.

100 Deals associated with KST-016366

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