Catalog No.S2700 Synonyms: KX 01
Molecular Weight(MW): 431.53
KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.
Cited by 16 Publications
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Images of typical cultures treated with the compounds and/or 500 pM BoNT/A. Cells were treated with the compounds for 30 min and then intoxicated with 500 pM BoNT/A for 4 h. Cells were then fixed and immunostained for neuron-specific b-III Tubulin (green) and Hoechst dye (nuclei; blue).
Neurotox Res, 2015, 27(4):384-98.. KX2-391 purchased from Selleck.
The histogram represents the absolute cell numbers obtained after 15 days of culture, in the presence of KX2-391 inhibitor at different concentrations and Dasatinib, as compared to control, arbitrarily normalized to one. The data are represented as mean±SEM obtained by nine independent experiments and analyzed by Wilcoxon signed-rank test (*p < 0.05; **p < 0.005).
Front Immunol, 2018, 9:2433. KX2-391 purchased from Selleck.
(A) MDA-pc3, and MDA-B6 cells were cultured in glass-bottom plates in the presence of 25 nM KX2-391 or DMSO for 72 h and stained with 2.7 µg/mL propidium iodide (PI) in phenol red-free medium. Stained cells were imaged at 200 x magnification using Zeiss LSM 700 confocal microscope and PI-stained cells were counted in at least 10 randomly captured frames. Counts of PI-positive cells were normalized on the total cell numbers in matching frames. The graph shows the ratio of PI-positive cells in KX2-391-treated populations relative to matching DMSO controls.
Oncotarget, 2016, 7(31):50027-50042. KX2-391 purchased from Selleck.
Inhibition of Src activity increases the frequency of c-H2AX foci formation in adjacent nonirradiated bystander cells. Cells were treated with Src inhibitor Kx2-391 (final concentration 2 nM) for 1 h and removed before irradiation. At 4 h after 50 cGy a irradiation, cells were fixed for c-H2AX immunofluorescence staining (scale bar, 10 lm). Panel A: Level of c-H2AX foci formation in adjacent nonirradiated cells. Panel B: Level of c-H2AX foci formation in directly irradiated cells. Data were pooled from three independent experiments, and the results are presented as mean 6 SD. *P , 0.05, **P , 0.01, ***P , 0.001. NS ¼ not significant
Radiat Res, 2018, 190(5):494-503. KX2-391 purchased from Selleck.
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|Description||KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 2.|
KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM), and HepG2 (GI 50 = 60 nM), four hepatic cell cancer (HCC) cell lines.  KX2-391 is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. KX2-391 is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively. 
|In vivo||In pre-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis. |
|In vitro||DMSO||86 mg/mL (199.29 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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Frequently Asked Questions
How to formulate KX2-391 for animal trials?
KX2-391 can be dissolved in 4% DMSO/corn oil at 5 mg/ml as a homogeneous suspension for oral administration and dissolved in 4% DMSO/30% PEG 300/ddH2O at 5 mg/ml as a clear solution.