KX2-361 free base
KX2-361 is a Src-kinase and tubulin polymerization inhibitor.
For research use only. Not for human or veterinary use.
KX2-361 structure
CAS No.: 897016-26-1
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| No pack sizes listed. Request a quote. | ||||
Description
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.
Biological activity
In Vitro 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 In Vivo 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
Identifiers
- SMILES
-
O=C(NCC=1C=CC=C(F)C1)CC=2N=CC(=CC2)C3=CC=C(C=C3)N4CCOCC4 - InChIKey
-
CMKKPJNMYLOUCE-UHFFFAOYSA-N
Specifications
- MW (average)
- 405.4647
- Formula
- C24H24FN3O2
- CAS No.
- 897016-26-1
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder 4°C, protect from light; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO
- In vitro
- DMSO : 10.71 mg/mL