KX2-391

Catalog No.S2700 Synonyms: KX 01

KX2-391 Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 90 In stock
USD 170 In stock
USD 570 In stock
USD 970 In stock
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Cited by 8 Publications

5 Customer Reviews

  • 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.

    MDA-MB-231 cells were treated with KX2-391 for 12 h followed by immunoblotting analysis. Densitometric data (fold) were shown below each group.

    Acta Pharmacol Sin, 2018, 39(8):1326-1337. 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.

Purity & Quality Control

Choose Selective Src Inhibitors

Biological Activity

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.
Targets
Src (HuH7) [1]
(Cell-free assay)
Src (PLC/PRF/5) [1]
(Cell-free assay)
Src (Hep 3B) [1]
(Cell-free assay)
Src (Hep G2) [1]
(Cell-free assay)
9 nM(GI50) 13 nM(GI50) 26 nM(GI50) 60 nM(GI50)
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 (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. [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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
mouse NIH3T3 cells NGrPVnhHfW6ldHnvckBie3OjeR?= MnjHN{Bl[Xm| MX\Jcohq[mm2aX;uJI9nKGOxboP0bZR2fGm4ZXz5JIFkfGm4ZTDoeY1idiClLWPSR|UzP0ZibYX0ZY51NWmwZIXj[YQh\3Kxd4ToJIlvcGmkaYTpc44hcW5ibX;1d4UhVkmKM2SzJINmdGy|IHHmeIVzKDNiZHH5d{BjgSCPVGSgZZN{[Xl? MoHSNlE5PTJyMkO=

... Click to View More Cell Line Experimental Data

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

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: Huh7, PLC/PRF/5, Hep3B, and HepG2 cell lines
  • Concentrations: 6,564 to 0.012 nM
  • Incubation Time: 3 days
  • Method:

    Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 (NutriCyte, Buffalo, NY) 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 microliters 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 by using BioTek Synergy HT multiplatform microplate reader. 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.</


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (199.29 mM)
Water Insoluble
Ethanol Insoluble
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.
5mg/mL

* 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.

Chemical Information

Molecular Weight 431.53
Formula

C26H29N3O3

CAS No. 897016-82-9
Storage powder
in solvent
Synonyms KX 01

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03575780 Recruiting Actinic Keratoses Athenex Inc.|TKL Research Inc. September 7 2018 Phase 1
NCT03575780 Recruiting Actinic Keratoses Athenex Inc.|TKL Research Inc. September 7 2018 Phase 1
NCT03285490 Active not recruiting Actinic Keratosis Athenex Inc. September 15 2017 Phase 3
NCT03285477 Active not recruiting Actinic Keratoses Athenex Inc. September 15 2017 Phase 3
NCT03285490 Active not recruiting Actinic Keratosis Athenex Inc. September 15 2017 Phase 3
NCT03285477 Active not recruiting Actinic Keratoses Athenex Inc. September 15 2017 Phase 3

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    How to formulate KX2-391 for animal trials?

  • Answer:

    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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID