An Src kinase inhibitor with strong anticancer properties (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma

KX2-391 – 50 mg

Brand:
Cayman
CAS:
897016-82-9
Storage:
-20
UN-No:
Non-Hazardous - /

KX2-391 is a highly selective and potent Src kinase inhibitor with strong anticancer properties that binds specifically to the substrate binding site of Src kinase (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma, respectively; GI50 = 9, 13, 26, and 60 nM in HuH7, PLC/PRF/5, Hep 3B, and Hep G2 hepatocellular carcinoma cell lines, respectively).{33784,33783,33781} It does not affect PDGFR, EGFR, JAK1, JAK2, Lck, or ZAP-70.{33780,33782} In ERα positive breast cancer cells, KX2-391 induced apoptosis through activation of caspases 6, 7, 8, and 9.{33780} It can also induce p53 expression and stimulate caspase-3 and PARP cleavage in vitro.{33784} KX2-391 has been through Phase I and Phase II clinical trials for patients with acute myeloid leukemia, solid tumors, prostate cancers, and lymphoma.{33784,33781} A Phase II clinical trial is ongoing for a formulation of KX2-391 in ointment form for patients with actinic keratosis, a disorder of the skin that can lead to squamous cell carcinoma.  

 

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Description

An Src kinase inhibitor with strong anticancer properties (IC50 = 20 nM for Src kinase autophosphorylation; IC50 = 100 nM and 25 nM in human tumor cells in the presence and absence of human plasma, respectively; GI50 = 9, 13, 26, and 60 nM in HuH7, PLC/PRF/5, Hep 3B, and Hep G2 hepatocellular carcinoma cell lines, respectively)

Formal name: 5-[4-[2-(4-morpholinyl)ethoxy]phenyl]-N-(phenylmethyl)-2-pyridineacetamide

Synonyms:  KX 01

Molecular weight: 431.5

CAS: 897016-82-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|SRC Family Signaling

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