Tirbanibulin Mesylate

SKU: orb1219122

Description

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

Key Properties

• CAS Number: 1080645-95-9
• MW: 527.63
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₃N₃O₆S
• SMILES: O=C(NCC1=CC=CC=C1)CC2=NC=C(C3=CC=C(OCCN4CCOCC4)C=C3)C=C2.OS(=O)(C)=O
• Target: Src
• Solubility: DMSO:99 mg/mL (187.63 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Orally administered Tirbanibulin Mesylate (KX2-391 Mesylate) is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer.
• In Vitro:
  Tirbanibulin Mesylate (KX2-391 Mesylate) is a Src inhibitor that is directed to the Src substrate pocket. Tirbanibulin (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. Tirbanibulin Mesylate (KX2-391 Mesylate) 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. Tirbanibulin Mesylate (KX2-391 Mesylate) 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

KX2-391 Mesylate | KX01 Mesylate

Quick Database Links

Gene Symbol

Src