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=NC=C(C=C2)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

Molecular Formula	C24H24FN3O2
Molecular Weight	405.4647
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

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

Title	Date	PubMed
No data available in table

Substance Class	Chemical
Record UNII	RVW387BA9U
Record Status	`Validated (UNII)`
Record Version

Show entries

Name

Type

Language

KX2-361

Common Name

English

KX-02

Code

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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Related Record

Type

Details


					A718CYC1N0

KX2-361 BESYLATE

SALT/SOLVATE -> PARENT

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Related Record

Type

Details


					RVW387BA9U

KX2-361

ACTIVE MOIETY

Comments:

Originator: Kinex Pharmaceuticals; Developer: Athenex, Roswell Park Cancer Institute, Xiangxue Pharmaceutical; Class: Antineoplastic, Small molecule; Mechanism of Action: Src-Family kinase inhibitor, Tubulin polymerisation inhibitor; Orphan Drug Status: Yes for Glioma; On Fast track: No; New Molecular Entity: Yes; Highest Development Phases: Phase I for Glioma, Preclinical for Brain cancer; Most Recent Events: 24 Dec 2014 Phase-I clinical trials in Glioma (Metastatic disease) in USA (PO) (9173057, NCT02326441), 04 Dec 2013 KX 02 receives Orphan Drug status for Glioma in USA, 05 Jun 2013 FDA approves IND application for KX 02 in Glioma


					RVW387BA9U

KX2-361

ACTIVE MOIETY

Comments:

In a well-established glioblastoma multiforme (GBM) brain tumor syngeneic mouse model, KX02 consistently cures the mice of their brain tumors after four weeks of therapy in 30-60% of treated animals. These pre-clinical studies showed that KX02 induced more necrosis in the GBM tumors compared to Temodar, and also resulted in more immune cell infiltration into the tumor tissues. Pharmacokinetic studies showed that KX02 is absorbed orally and has facile penetration into brain tissue from plasma, providing even higher drug levels in the brain than the plasma. Athenex has received Orphan Drug designation for KX02 from the US FDA for the treatment of gliomas, which are the most common and aggressive form of brain cancer. Orphan drug status qualifies Athenex for seven years of exclusivity after formal marketing approval, as well as further development incentives. XiangXue Pharmaceuticals in Guangzhou, China, is the collaborative development partner for KX02 in China. As a part of that partnership, XiangXue is preparing an IND application for the Chinese FDA.

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