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.
2 Customer Reviews
(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.
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.
Purity & Quality Control
Choose Selective Src Inhibitors
|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:
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 (g) = Concentration (mol/L) × Volume (L) × 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
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02838628||Active, not recruiting||Actinic Keratosis||Kinex Pharmaceuticals Inc||April 2016||Phase 2|
|NCT02337205||Completed||Actinic Keratosis||Kinex Pharmaceuticals Inc||December 2014||Phase 1|
|NCT01397799||Completed||Acute Myelogenous Leukemia||Kinex Pharmaceuticals Inc||December 2013||Phase 1|
|NCT01764087||Unknown status||Unspecified Adult Solid Tumor, Protocol Specific|Gastric Cancer|Breast Cancer||Hanmi Pharmaceutical Company Limited||December 2012||Phase 1|Phase 2|
|NCT01074138||Completed||Bone-Metastatic, Castration-Resistant Prostate Cancer||Kinex Pharmaceuticals Inc||February 2010||Phase 2|
|NCT00658970||Completed||Solid Tumors|Lymphoma||Kinex Pharmaceuticals Inc||November 2007||Phase 1|
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.