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

KX2-391 Mesylate (Synonyms: KX01 Mesylate)

Cat. No.: HY-10340B Purity: 99.97%
Data Sheet SDS 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

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10 mM * 1 mL in DMSO $81 In-stock
5 mg $70 In-stock
10 mg $120 In-stock
50 mg $470 In-stock
100 mg $800 In-stock
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Description

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].

References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Cell Assay
[1]

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.

References
M.Wt

527.63

Formula

C₂₇H₃₃N₃O₆S

CAS No.

1080645-95-9

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

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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Product Name:
KX2-391 Mesylate
Cat. No.:
HY-10340B
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