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)
| Molecular Formula | C24H24FN3O2 |
| Molecular Weight | 405.4647 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| KX2-361: a novel orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma. | 2018 Dec |
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| Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361). | 2018 Jun 14 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:28:31 GMT 2023
by
admin
on
Sat Dec 16 11:28:31 GMT 2023
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| Record UNII |
RVW387BA9U
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| Record Status |
Validated (UNII)
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| Record Version |
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897016-26-1
Created by
admin on Sat Dec 16 11:28:31 GMT 2023 , Edited by admin on Sat Dec 16 11:28:31 GMT 2023
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KX2-361
Created by
admin on Sat Dec 16 11:28:31 GMT 2023 , Edited by admin on Sat Dec 16 11:28:31 GMT 2023
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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) | ||
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RVW387BA9U
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admin on Sat Dec 16 11:28:31 GMT 2023 , Edited by admin on Sat Dec 16 11:28:31 GMT 2023
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C120101
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admin on Sat Dec 16 11:28:31 GMT 2023 , Edited by admin on Sat Dec 16 11:28:31 GMT 2023
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KX2-361
Created by
admin on Sat Dec 16 11:28:31 GMT 2023 , Edited by admin on Sat Dec 16 11:28:31 GMT 2023
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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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11545920
Created by
admin on Sat Dec 16 11:28:31 GMT 2023 , Edited by admin on Sat Dec 16 11:28:31 GMT 2023
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |
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
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ACTIVE MOIETY |
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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