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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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500mg |
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Purity: ≥98%
Cevipabulin (formerly D-06576; TTI-237) is a triazolopyrimidine based microtubule targeting agent/tubulin inhibitor with potential antitumor activity. It differs from other vinca alkaloid compounds in that it acts via a novel mechanism. TTI-237 functions by selectively attaching to tubulin's vinca site, which encourages tubulin polymerization into microtubules. TTI-237 functions as a stabilizer, preventing microtubule disintegration and stabilizing tubulin.
Targets |
microtubule (IC50 = 18-40 nM)
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ln Vitro |
Cevipabulin (0-50 nM, 72 hours) exhibits good activity on cell lines from tumors of the ovary, breast, prostate, and cervical regions (between 18 and 40 nM IC50 values)[1].
Cevipabulin (TTI-237) generates sub-G1 nuclei at low concentrations (20–40 nM) and strongly inhibits the G2-M complex at higher concentrations (>50 nM), according to flow cytometry experiments[1]. |
ln Vivo |
Cevipabulin (TTI-2370)( 5, 10, 15, and 20 mg/kg, every 4 days for 4 cycles, in mice) is effective against human tumor xenografts when administered intravenously and orally, exhibiting dose-dependent effects and strong antitumor activity at doses of 20 and 15 mg/kg[1].
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Cell 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. |
Animal Protocol |
Athymic nu/nu female mice implanted s.c. in the flank with 1×107 LoVo human colon adenocarcinoma cells[1]
5, 10, 15, and 20 mg/kg I.V. injection every 4 days for 4 cycles. |
References |
Molecular Formula |
C18H18CLF5N6O
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Molecular Weight |
464.82
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Exact Mass |
464.11508
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Elemental Analysis |
C, 46.51; H, 3.90; Cl, 7.63; F, 20.44; N, 18.08; O, 3.44
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CAS # |
849550-05-6
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Related CAS # |
Cevipabulin fumarate;849550-67-0
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Appearance |
solid powder
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SMILES |
C[C@@H](C(F)(F)F)NC1=C(C(=NC2=NC=NN12)Cl)C3=C(C=C(C=C3F)OCCCNC)F
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InChi Key |
ZUZPCOQWSYNWLU-VIFPVBQESA-N
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InChi Code |
InChI=1S/C18H18ClF5N6O/c1-9(18(22,23)24)28-16-14(15(19)29-17-26-8-27-30(16)17)13-11(20)6-10(7-12(13)21)31-5-3-4-25-2/h6-9,25,28H,3-5H2,1-2H3/t9-/m0/s1
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Chemical Name |
5-chloro-6-[2,6-difluoro-4-[3-(methylamino)propoxy]phenyl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]-[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
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Synonyms |
Cevipabulin; TTI 237; TTI237; TTI-237; D06576; D-06576; D 06576
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~16.7 mg/mL (35.9 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.67 mg/mL (3.59 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (3.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT00195325 | Terminated | Drug: TTI-237 | Tumors Neoplasms |
Wyeth is now a wholly owned subsidiary of Pfizer |
August 2005 | Phase 1 |
NCT00195247 | Terminated | Drug: TTI-237 Neoplasms |
Neoplasms | Wyeth is now a wholly owned subsidiary of Pfizer |
May 2005 | Phase 1 |