Tipifarnib - 98%, high purity , CAS No.192185-72-1, Inhibitor of farnesyltransferase; CAAX box; beta

Item Number
T125396
Grouped product items
SKUSizeAvailabilityPrice Qty
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

Basic Description

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
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsTipifarnib 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 TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor 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.

Associated Targets(Human)

FNTB Tclin Protein farnesyltransferase subunit beta (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 6-[(R)-amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one
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

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

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9 results found

Lot NumberCertificate TypeDateItem
I2404220Certificate of AnalysisAug 22, 2024 T125396
I2404221Certificate of AnalysisAug 22, 2024 T125396
I2404433Certificate of AnalysisAug 22, 2024 T125396
A2219621Certificate of AnalysisNov 10, 2023 T125396
A2219623Certificate of AnalysisNov 10, 2023 T125396
A2219692Certificate of AnalysisNov 10, 2023 T125396
A2219693Certificate of AnalysisNov 10, 2023 T125396
A2219694Certificate of AnalysisNov 10, 2023 T125396
A2219741Certificate of AnalysisNov 10, 2023 T125396

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 48.94, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 9.79, Max Conc. mM: 20

Safety and Hazards(GHS)

Pictogram(s) GHS07
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.

Related Documents

References

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,  (10): (1095-102).  [PMID:12769710]
3. Downward J.  (2003)  Targeting RAS signalling pathways in cancer therapy..  Nat Rev Cancer,  (1): (11-22).  [PMID:12509763]

Solution Calculators