1. Cell Cycle/DNA Damage
    Cytoskeleton
  2. Microtubule/Tubulin

Cevipabulin (Synonyms: TTI-237)

Cat. No.: HY-14949 Purity: 98.09%
Data Sheet SDS Handling Instructions

Cevipabulin(TTI-237) is a novel, potent, synthetic small molecule, inhibits binding of vinblastine at the Vinca alkaloid site of the αβ-tubulin heterodimer.

For research use only. We do not sell to patients.
Cevipabulin Chemical Structure

Cevipabulin Chemical Structure

CAS No. : 849550-05-6

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $154 In-stock
5 mg $140 In-stock
10 mg $240 In-stock
50 mg $740 In-stock
100 mg $950 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Cevipabulin(TTI-237) is a novel, potent, synthetic small molecule, inhibits binding of vinblastine at the Vinca alkaloid site of the αβ-tubulin heterodimer. IC50 value: Target: Antimicrotubule agent in vitro: TTI-237 inhibited the binding of [(3)H]vinblastine to tubulin, but it caused a marked increase in turbidity development that more closely resembled the effect observed with docetaxel than that observed with vincristine. When applied to cultured human tumor cells at concentrations near its IC(50) value for cytotoxicity (34 nmol/L), TTI-237 induced multiple spindle poles and multinuclear cells, as did paclitaxel, but not vincristine or colchicine. Flow cytometry experiments revealed that, at low concentrations (20-40 nmol/L), TTI-237 produced sub-G(1) nuclei and, at concentrations above 50 nmol/L, it caused a strong G(2)-M block. The compound was a weak substrate of multidrug resistance 1 (multidrug resistance transporter or P-glycoprotein). In a cell line expressing a high level of P-glycoprotein, the IC(50) of TTI-237 increased 25-fold whereas those of paclitaxel and vincristine increased 806-fold and 925-fold, respectively. TTI-237 was not recognized by the MRP or MXR transporters [1]. TTI-237 inhibited the exchange of [(3)H]GTP at the exchangeable nucleotide site of the tubulin heterodimer, and was similar to vincristine in its effects on the phosphorylation of eight intracellular proteins in HeLa cells [3]. in vivo: TTI-237 was active in vivo in several nude mouse xenograft models of human cancer, including LoVo human colon carcinoma and U87-MG human glioblastoma, when dosed i.v. or p.o [1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00195325 Wyeth is now a wholly owned subsidiary of Pfizer Tumors|Neoplasms August 2005 Phase 1
NCT00195247 Wyeth is now a wholly owned subsidiary of Pfizer Neoplasms May 2005 Phase 1
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References
Molecular Weight

464.82

Formula

C₁₈H₁₈ClF₅N₆O

CAS No.

849550-05-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 10 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Cevipabulin
Cat. No.:
HY-14949
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