Catalog No.S2700 Synonyms: KX 01
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.
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|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.|
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.  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. 
|In vivo||In pre-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis. |
|In vitro||DMSO||86 mg/mL (199.29 mM)|
|In vivo||4% DMSO+30% PEG 300+ddH2O||5mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02838628||Active, not recruiting||Actinic Keratosis||Kinex Pharmaceuticals Inc||April 2016||Phase 2|
|NCT02337205||Completed||Actinic Keratosis||Kinex Pharmaceuticals Inc||December 2014||Phase 1|
|NCT01397799||Completed||Acute Myelogenous Leukemia||Kinex Pharmaceuticals Inc||December 2013||Phase 1|
|NCT01764087||Unknown status||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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