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

Cevipabulin (Synonyms: TTI-237)

Cat. No.: HY-14949 Purity: 99.03%
Handling Instructions

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.

For research use only. We do not sell to patients.

Cevipabulin Chemical Structure

Cevipabulin Chemical Structure

CAS No. : 849550-05-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 185 In-stock
Estimated Time of Arrival: December 31
5 mg USD 168 In-stock
Estimated Time of Arrival: December 31
10 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 888 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1140 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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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[1][2].

IC50 & Target

IC50: 18-40 nM (microtubule in human tumor cells)[1].

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[1].
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[1].

Cell Cytotoxicity Assay[1]

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.
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[1].

Animal Model: Athymic nu/nu female mice implanted s.c. in the flank with 1×107 LoVo human colon adenocarcinoma cells[1]
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[1].
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.
Clinical Trial
Molecular Weight

464.82

Formula

C₁₈H₁₈ClF₅N₆O

CAS No.

849550-05-6

SMILES

C[[email protected]@]([H])(C(F)(F)F)NC1=C(C2=C(F)C=C(OCCCNC)C=C2F)C(Cl)=NC3=NC=NN13

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 16.67 mg/mL (35.86 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1514 mL 10.7569 mL 21.5137 mL
5 mM 0.4303 mL 2.1514 mL 4.3027 mL
10 mM 0.2151 mL 1.0757 mL 2.1514 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (3.59 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.67 mg/mL (3.59 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (3.59 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.03%

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Keywords:

CevipabulinTTI-237TTI237TTI 237Microtubule/TubulinInhibitorinhibitorinhibit

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