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Tirbanibulin dihydrochloride

Catalog No. T15674   CAS 1038395-65-1
Synonyms: KX-01 (dihydrochloride), KX2-391 (dihydrochloride)

Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).

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Tirbanibulin dihydrochloride Chemical Structure
Tirbanibulin dihydrochloride, CAS 1038395-65-1
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Tirbanibulin is an inhibitor of Src that targets the peptide substrate site of Src (GI50: 9-60 nM in cancer cell lines).
Targets&IC50 Src HepG2:60 nM, Src PLC/PRF/5:13 nM, Src HuH7:(GI50)9 nM, Src Hep3B:26 nM
In vitro Tirbanibulin (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 displays 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]. Tirbanibulin 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, Tirbanibulin (p.o.) is shown to inhibit primary tumor growth and to suppress metastasis[2].
Synonyms KX-01 (dihydrochloride), KX2-391 (dihydrochloride)
Molecular Weight 504.45
Formula C26H31Cl2N3O3
CAS No. 1038395-65-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33.33 mg/mL (66.07 mM), sonification is recommended.

TargetMolReferences and Literature

1. Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig Dis Sci, 2009, 54(7), 1465-1474. 2. Fallah-Tafti A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur J Med Chem, 2011, 46(10), 4853-4858.

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Keywords

Tirbanibulin dihydrochloride 1038395-65-1 Angiogenesis Tyrosine Kinase/Adaptors Src Tirbanibulin Tirbanibulin Dihydrochloride KX2-391 KX 01 KX-01 KX-01 (dihydrochloride) KX01 KX2-391 (dihydrochloride) inhibitor inhibit

 

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