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KX02 (KX-02; KX2-361; KX2361) is a novel, orally bioavailable and potent dual inhibitor of both Src kinase and tubulin with potential antitumor activity.
| ln Vitro |
In GL261 cells, KX2-361 (0-200 nM, 24-72 hours) decreases Src autophosphorylation [1]. U87 cells are stimulated in the G2/M phase of the cell cycle by KX2-361 (0-270 nM). T98G, GL261, and U87 cell lines all exhibit indicator lights when exposed to KX2-361 (0-800 nM)[1]. Proteins that polymerize microtubules are inhibited by KX2-361 (5 µM). Keep in mind that after 270 nM, coupling effects totally end [1]. The ontological structure of entities [1].
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| ln Vivo |
Long-term survival is achieved and the growth of orthotopic GL261 brain tumors is greatly delayed by KX2-361 [1]. KX2-361 showed substantial brain penetration in mice given the lung cancer medication (20 mg/kg), with an observed brain Cmax of 4025±319 ng/g and a total exposure (AUClast) of 5044± 15 minutes post-pregnancy 355 h ng/g[1].
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| References | |
| Additional Infomation |
Src/tubulin Inhibitor 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 KX2-361 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. Src, a non-receptor tyrosine kinase, is overexpressed in a variety of tumor cell types and plays a key role in tumor cell proliferation, angiogenesis, migration, and metastasis.
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| Molecular Formula |
C24H24FN3O2
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|---|---|
| Molecular Weight |
405.4734
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| Exact Mass |
405.185
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| CAS # |
897016-26-1
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| Related CAS # |
897016-26-1;1571072-87-1 (besylate);
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| PubChem CID |
11545920
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
660.1±55.0 °C at 760 mmHg
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| Flash Point |
353.0±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.598
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| LogP |
2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
535
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CMKKPJNMYLOUCE-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
N-[(3-fluorophenyl)methyl]-2-[5-(4-morpholin-4-ylphenyl)pyridin-2-yl]acetamide
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| Synonyms |
KX-2-361 KX 02 KX2-361 KX02 KX-02KX 2-361
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4663 mL | 12.3314 mL | 24.6627 mL | |
| 5 mM | 0.4933 mL | 2.4663 mL | 4.9325 mL | |
| 10 mM | 0.2466 mL | 1.2331 mL | 2.4663 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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