1. Protein Tyrosine Kinase/RTK
    Cell Cycle/DNA Damage
  2. Src

KX2-391 Mesylate (Synonyms: KX01 Mesylate)

Cat. No.: HY-10340B Purity: 99.97%
Handling Instructions

KX2-391 Mesylate is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

For research use only. We do not sell to patients.
KX2-391 Mesylate Chemical Structure

KX2-391 Mesylate Chemical Structure

CAS No. : 1080645-95-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 98 In-stock
5 mg USD 84 In-stock
10 mg USD 144 In-stock
50 mg USD 564 In-stock
100 mg USD 960 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of KX2-391 Mesylate:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


KX2-391 Mesylate is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

IC50 & Target

GI50: 9 nM (Src, in HuH7 cells), 13 nM (Src, in PLC/PRF/5 cells), 26 nM (Src, in Hep3B cells), 60 nM (Src, in HepG2 cells)[1]

In Vitro

KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI50=9 nM), PLC/PRF/5 (GI50=13 nM), Hep3B (GI50=26 nM), and HepG2 (GI50=60 nM), four hepatic cell cancer (HCC) cell lines[1]. 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[2].

In Vivo

Orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer[2].

Clinical Trial
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.8953 mL 9.4763 mL 18.9527 mL
5 mM 0.3791 mL 1.8953 mL 3.7905 mL
10 mM 0.1895 mL 0.9476 mL 1.8953 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay

KX2-391 is prepared in DMSO and stored, and then diluted with appropriate medium before use[1].

Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 are routinely cultured and maintained in basal medium containing 2% fetal bovine serum (FBS) at 37°C and 5% CO2. Cells are seeded at 4.0×103/190 μL and 8.0×103/190 μL per well of 96-well plate in basal medium containing 1.5% FBS. These are cultured overnight at 37°C and 5% CO2 prior to the addition of KX2-391, at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten μLs of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/mL) is then added to each well on day 3 and cells incubated for 4 hours. The formazan product is dissolved with 10% SDS in dilute HCl. Optical density at 570 nm is measured. For comparison of activity and potency, parallel experiments are performed using KX2-391. Growth inhibition curves, 50% inhibition concentration (GI50), and 80% inhibition concentration (GI80) are determined using GraphPad Prism 5 statistical software. Data are normalized to represent percentage of maximum response as well as reported in optical density at wavelength of 570 nm (OD570) signal format. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight









-20°C, protect from light, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.


Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 57 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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