Cevipabulin

SKU: orb2901833

Description

Cevipabulin (TTI-237) is an oral, microtubule-active antitumor compound and inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line.

Key Properties

• CAS Number: 849550-05-6
• MW: 464.82
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₈ClF₅N₆O
• SMILES: [H][C@@](C)(Nc1c(c(Cl)nc2ncnn12)-c1c(F)cc(OCCCNC)cc1F)C(F)(F)F
• Solubility: In Vitro: DMSO : 16.67 mg/mL (35.86 mM; Ultrasonic )

Bioactivity

• In Vivo:
  Cevipabulin (TTI-2370)(5, 10, 15, and 20 mg/kg, every 4 days for 4 cycles, in mice) is active by i. v. and p.o. administration against human tumor xenografts, showing dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg. Animal model: Athymic nu/nu female mice implanted s. c. in the flank with 1×107 LoVo human colon adenocarcinoma cells. Dosage: 5, 10, 15, and 20 mg/kg. Administration: I. V. injection every 4 days for 4 cycles. Result: The compound showed dose-dependent effects, with good antitumor activity at 20 and 15 mg/kg. Animal model: Athymic nu/nu female mice implanted s. c. in the flank with 1×106 U87-MG human glioblastoma cells. Dosage: 25 mg/kg. Administration: p.o. or I. V. Result: The compound was active by p.o. or i. v. administration against human tumor xenografts.
• In Vitro:
  Cevipabulin (0-50 nM, 72 hours) shows good activity (between 18 and 40 nM IC50 values) on cell lines from ovarian, breast, prostate, and cervical tumors. Flow cytometry experiments reveal that, Cevipabulin (TTI-237) at low concentrations (20-40 nM) produces sub-G1 nuclei and, at concentrations above 50 nM, it causes a strong G2-M block. Cell Cytotoxicity Assay Cell line: Human cancer cell lines (SK-OV-3, MDA-MB-435, MDA-MB-468, LnCaP, and Hela cells). Concentration: 0-50 nM. Incubation time: 72 hours. Result: The IC50 values are 24±8 nM, 21±4 nM, 18±6 nM, 22±7 nM and 40 nM in SK-OV-3, MDA-MB-435, MDA-MB-468, LnCaP and Hela cells.

Storage & Handling

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