KX2-391

Catalog No.S2700

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.

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KX2-391 Chemical Structure

KX2-391 Chemical Structure
Molecular Weight: 431.53

Validation & Quality Control

Quality Control & MSDS

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Product Information

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Product Description

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)
IC50 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]
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]
Features

Protocol(Only for Reference)

Cell Assay:

[1]

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.</

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Lau GM, et al, Dig Dis Sci, 2009, 54(7), 1465-1474.

[2] Fallah-Tafti A, et al, Eur J Med Chem, 2011, 46(10), 4853-4858.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02337205 Active, not recruiting Actinic Keratosis Kinex Pharmaceuticals Inc December 2014 Phase 1
NCT01397799 Completed Acute Myelogenous Leukemia Kinex Pharmaceuticals Inc December 2013 Phase 1
NCT01764087 Recruiting 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

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Chemical Information

Download KX2-391 SDF
Molecular Weight (MW) 431.53
Formula

C26H29N3O3

CAS No. 897016-82-9
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms KX 01
Solubility (25°C) * In vitro DMSO 86 mg/mL (199.29 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 4% DMSO+30% PEG 300+ddH2O 5mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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 Name N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide

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.

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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