| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Animal Protocol |
Pharmacokinetic Study in Mice:** **Tipifarnib** was suspended at 10 mg/mL in 20% (w/v) hydroxypropyl betacyclodextrin solution. BALB/c mice (7-8 week old females, ~20 g) received a single oral dose of 50 mg/kg via gavage (100 µL volume). Blood samples were collected from the tail at timed intervals. Plasma was separated and analyzed by LC-MS/MS to determine drug concentration. [1]
**Efficacy Study in Mice (Chagas Disease Model):** BALB/c mice were infected subcutaneously with 5 x 10³ *T. cruzi* trypomastigotes (Tulahuen strain). Treatment began on day 8 post-infection. For **tipifarnib**, mice were initially dosed at 100 mg/kg twice daily (days 8-13), but due to observed weight loss, the dose was reduced to 50 mg/kg twice daily for days 14-27. The drug was administered by oral gavage. Parasitemia was monitored by microscopic examination of tail blood. Mice that became moribund were euthanized. [1] |
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| References | |
| Additional Infomation |
6-[(S)-amino-(4-chlorophenyl)-(3-methyl-4-imidazolyl)methyl]-4-(3-chlorophenyl)-1-methyl-2-quinolinone is a diarylheptane compound.
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| Molecular Formula |
C27H22CL2N4O
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|---|---|
| Molecular Weight |
489.4
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| Exact Mass |
488.117
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| Elemental Analysis |
C, 66.26; H, 4.53; Cl, 14.49; N, 11.45; O, 3.27
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| CAS # |
192185-71-0
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| Related CAS # |
Tipifarnib;192185-72-1
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| PubChem CID |
9935249
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| Appearance |
White to light yellow solid powder
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| LogP |
6.196
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
34
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| Complexity |
785
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C1N(C)C2=C(C=C([C@](C3=CC=C(Cl)C=C3)(N)C4=CN=CN4C)C=C2)C(C5=CC=CC(Cl)=C5)=C1
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| InChi Key |
PLHJCIYEEKOWNM-MHZLTWQESA-N
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| InChi Code |
InChI=1S/C27H22Cl2N4O/c1-32-16-31-15-25(32)27(30,18-6-9-20(28)10-7-18)19-8-11-24-23(13-19)22(14-26(34)33(24)2)17-4-3-5-21(29)12-17/h3-16H,30H2,1-2H3/t27-/m0/s1
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| Chemical Name |
6-[(S)-amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one
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| Synonyms |
(S)-Tipifarnib; (S)-Zarnestra
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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: ~25 mg/mL (~51.1 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.11 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 25.0 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: ≥ 2.5 mg/mL (5.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0433 mL | 10.2166 mL | 20.4332 mL | |
| 5 mM | 0.4087 mL | 2.0433 mL | 4.0866 mL | |
| 10 mM | 0.2043 mL | 1.0217 mL | 2.0433 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.
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