KX2-361

• CAT Number: I007544
• CAS Number: 897016-26-1
• Molecular Formula: C24H24FN3O2
• Molecular Weight: 405.46
• Purity: ≥95%
• Synonyms: N-[(3-fluorophenyl)methyl]-2-[5-(4-morpholin-4-ylphenyl)pyridin-2-yl]acetamide
• InChI: 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)
• InChIKey: CMKKPJNMYLOUCE-UHFFFAOYSA-N
• SMILES: C1COCCN1C2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC(=CC=C4)F

KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell[1].
KX2-361 (0-200 nM, 24-72 h) reduces autophosphorylation of Src in GL261 cells[1].
KX2-361 (0-270 nM) promotes cell cycle arrest at the G2/M phase in U87 cells. Note the dose dependent effect and virtual complete arrest at 270 nM[1].
KX2-361 (0-800 nM) induces apoptosis of U87, GL261 and T98G cell lines[1].
KX2-361 (5 µM) inhibits the in vitro assembly of tubulin polymers[1].
KX2‑361 significantly delays progression of orthotopic GL261 brain tumors and produces long‑term survival[1].
KX2-361 demonstrates appreciable brain penetration when dosed orally to mice (20 mg/kg), with a brain Cmax of 4025±319 ng/g observed 15 min post-dosing and an overall exposure (AUClast) of 5044±355 h ng/g[1].

Reference

[1]. Ciesielski MJ, et al. KX2-361: a novel orally bioavailable small molecule dual Src/tubulin inhibitor that provides long term survival in a murine model of glioblastoma. J Neurooncol. 2018 Dec;140(3):519-527.
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