KX2-361

Investigational

Details

Stereochemistry	ACHIRAL
Molecular Formula	C24H24FN3O2
Molecular Weight	405.4647
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

FC1=CC=CC(CNC(=O)CC2=CC=C(C=N2)C3=CC=C(C=C3)N4CCOCC4)=C1

InChI

InChIKey=CMKKPJNMYLOUCE-UHFFFAOYSA-N

InChI=1S/C24H24FN3O2/c25-21-3-1-2-18(14-21)16-27-24(29)15-22-7-4-20(17-26-22)19-5-8-23(9-6-19)28-10-12-30-13-11-28/h1-9,14,17H,10-13,15-16H2,(H,27,29)

HIDE SMILES / InChI

Description

KX-02 is a compound demonstrating dual inhibitory activity against Src kinase and tubulin polymerization. It readily crosses the blood-brain-barrier in mice. It is under development for the treatment of solid tumors.

CNS Activity

Originator

Approval Year

PubMed

PubMed

Show entries

Title	Date	PubMed
Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361).	2018 Jun 14	29617135

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Name

Type

Language

KX2-361

Common Name

English

KX-02

Preferred Name

English

2-PYRIDINEACETAMIDE, N-((3-FLUOROPHENYL)METHYL)-5-(4-(4-MORPHOLINYL)PHENYL)-

Systematic Name

English

KX-2361

Code

English

N-(3-FLUOROBENZYL)-2-(5-(4-MORPHOLINOPHENYL) PYRIDIN-2-YL) ACETAMIDE

Systematic Name

English

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Code System

Code

Type

Description

CAS

897016-26-1

PRIMARY

MANUFACTURER PRODUCT INFORMATION

KX2-361

PRIMARY

MedKoo CAT NO.: 206196; CAS NO.: 897016-26-1Description: KX02, also known as KX2-361, is a lipophilic, orally available inhibitor of both Src kinase activity and tubulin polymerization, with potential antineoplastic activity. Upon oral administration, src/tubulin inhibitor KX02 binds to and inhibits the activity of Src kinase. This inhibits both downstream signaling and the proliferation of Src kinase-expressing tumor cells. KX02 also binds to tubulin heterodimers and inhibits microtubule polymerization, thereby disrupting microtubule formation, mitosis, and further proliferation. (Last updated: 5/6/2016)

FDA UNII

RVW387BA9U

PRIMARY

NCI_THESAURUS

C120101

PRIMARY

CLINICAL_TRIALS.GOV

KX2-361

PRIMARY

Official Title: A Phase 1 Clinical Study to Evaluate the Safety, Tolerability and Pharmacokinetics of KX2-361 in Subjects With Advanced Malignancies That Are Refractory to Conventional TherapiesPurpose: The purpose of this study is to determine the safety and tolerability of the study drug KX2-361 and to determine how much of the study drug enters the bloodstream, in patients with advanced malignancies that have not responded to conventional therapies.

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ACTIVE MOIETY


					RVW387BA9U

KX2-361

SALT/SOLVATE (PARENT)


					A718CYC1N0

KX2-361 BESYLATE