KX2-361 (Synonyms: KX-02) |
| Catalog No.GC72824 |
KX2-361 (KX-02) es un inhibide la polimeride de src-quinasa y tubulina.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 897016-26-1
Sample solution is provided at 25 µL, 10mM.
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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.
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].
References:
[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.
| Cas No. | 897016-26-1 | SDF | |
| Sinónimos | KX-02 | ||
| Formula | C24H24FN3O2 | M.Wt | 405.46 |
| Solubility | DMSO : 10.71 mg/mL (26.41 mM; ultrasonic and warming and heat to 60°C) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4663 mL | 12.3317 mL | 24.6633 mL |
| 5 mM | 493.3 μL | 2.4663 mL | 4.9327 mL |
| 10 mM | 246.6 μL | 1.2332 mL | 2.4663 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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