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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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T125396-1mg | 1mg | In stock | $23.90 | |
T125396-5mg | 5mg | In stock | $72.90 | |
T125396-10mg | 10mg | In stock | $126.90 | |
T125396-25mg | 25mg | In stock | $239.90 | |
T125396-50mg | 50mg | In stock | $435.90 | |
T125396-100mg | 100mg | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $699.90 |
Potent farnesyltransferase inhibitor
Synonyms | (+)-(r)-6-[amino(4-chlorophenyl)(1-methyl-1h-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methyl-2(1h)-quinolinone | 6-[(R)-amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one | DS-14724 | HMS3748E21 | Q-102 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Tipifarnib is an orally active and potent farnesyltransferase (FTase) inhibitor that exhibits potent anti-tumorigenic effects. Tipifarnib mechanism of action is not fully understand. Inhibit the farnesylation of lamin B and K-RasB peptide substrates (IC50 |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of farnesyltransferase; CAAX box; beta |
Product Description | Pre-clinical studies show that tipifarnib has antiproliferative effects on pancreatic cancer cell lines at clinically relevant concentrations (concentration that inhibits 50% growth [IC50] from 9.5 to 500 nmol/L). It also exhibits marked growth retardation and antiangiogenic effects in a pancreatic cancer xenograft model. |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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IUPAC Name | 6-[(R)-amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one |
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INCHI | 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-/m1/s1 |
InChi Key | PLHJCIYEEKOWNM-HHHXNRCGSA-N |
Canonical SMILES | CN1C=NC=C1C(C2=CC=C(C=C2)Cl)(C3=CC4=C(C=C3)N(C(=O)C=C4C5=CC(=CC=C5)Cl)C)N |
Isomeric SMILES | CN1C=NC=C1[C@@](C2=CC=C(C=C2)Cl)(C3=CC4=C(C=C3)N(C(=O)C=C4C5=CC(=CC=C5)Cl)C)N |
PubChem CID | 159324 |
Molecular Weight | 489.4 |
PubChem CID | 159324 |
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CAS Registry No. | 192185-72-1 |
ChEMBL Ligand | CHEMBL289228 |
Wikipedia | Tipifarnib |
RCSB PDB Ligand | JAN |
Reactome Reaction | R-HSA-9647987 |
Reactome Drug | R-ALL-9647938 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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I2404220 | Certificate of Analysis | Aug 22, 2024 | T125396 |
I2404221 | Certificate of Analysis | Aug 22, 2024 | T125396 |
I2404433 | Certificate of Analysis | Aug 22, 2024 | T125396 |
A2219621 | Certificate of Analysis | Nov 10, 2023 | T125396 |
A2219623 | Certificate of Analysis | Nov 10, 2023 | T125396 |
A2219692 | Certificate of Analysis | Nov 10, 2023 | T125396 |
A2219693 | Certificate of Analysis | Nov 10, 2023 | T125396 |
A2219694 | Certificate of Analysis | Nov 10, 2023 | T125396 |
A2219741 | Certificate of Analysis | Nov 10, 2023 | T125396 |
Solubility | Solvent:DMSO, Max Conc. mg/mL: 48.94, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 9.79, Max Conc. mM: 20 |
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Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P271:Use only outdoors or in a well-ventilated area. P270:Do not eat, drink or smoke when using this product. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P330:Rinse mouth. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P317:IF SWALLOWED: Get medical help. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell. |
Starting at $79.90
1. End DW, Smets G, Todd AV, Applegate TL, Fuery CJ, Angibaud P, Venet M, Sanz G, Poignet H, Skrzat S et al.. (2001) Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro.. Cancer Res, 61 (1): (131-7). [PMID:11196150] |
2. Venet M, End D, Angibaud P. (2003) Farnesyl protein transferase inhibitor ZARNESTRA R115777 - history of a discovery.. Curr Top Med Chem, 3 (10): (1095-102). [PMID:12769710] |
3. Downward J. (2003) Targeting RAS signalling pathways in cancer therapy.. Nat Rev Cancer, 3 (1): (11-22). [PMID:12509763] |