1. Protein Tyrosine Kinase/RTK
    Cytoskeleton
    Cell Cycle/DNA Damage
  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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
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
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of KX2-391 Mesylate:

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01397799 Kinex Pharmaceuticals Inc Acute Myelogenous Leukemia December 2013 Phase 1
NCT01764087 Hanmi Pharmaceutical Company Limited Unspecified Adult Solid Tumor, Protocol Specific|Gastric Cancer|Breast Cancer December 2012 Phase 1|Phase 2
NCT02337205 Kinex Pharmaceuticals Inc Actinic Keratosis December 2014 Phase 1
NCT02838628 Kinex Pharmaceuticals Inc Actinic Keratosis April 2016 Phase 2
NCT01074138 Kinex Pharmaceuticals Inc Bone-Metastatic, Castration-Resistant Prostate Cancer February 2010 Phase 2
NCT00658970 Kinex Pharmaceuticals Inc Solid Tumors|Lymphoma November 2007 Phase 1
NCT00646139 Roswell Park Cancer Institute Lymphoma|Lymphoproliferative Disorder|Small Intestine Cancer|Unspecified Adult Solid Tumor, Protocol Specific October 2007 Phase 1
View MoreCollapse
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
M.Wt

527.63

Formula

C₂₇H₃₃N₃O₆S

CAS No.

1080645-95-9

Storage

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

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.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

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