KX2-361  (Synonyms: KX-02)

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

405.46

C₂₄H₂₄FN₃O₂

897016-26-1

Solid

White to off-white

O=C(NCC1=CC=CC(F)=C1)CC2=NC=C(C3=CC=C(N4CCOCC4)C=C3)C=C2

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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.  [Content Brief]