Tipifarnib

Tipifarnib
Clinical data
Other names	R115777
ATC code	None;
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name (+)-6-[(R)-Amino-(4-chlorophenyl)-(3-methylimidazol-4-yl)methyl]-4-(3-chlorophenyl)-1-methylquinolin-2-one;
CAS Number	192185-72-1 ;
PubChem CID	159324;
IUPHAR/BPS	8025;
DrugBank	DB04960 ;
ChemSpider	140122 ;
UNII	MAT637500A;
KEGG	D03720 ;
ChEBI	CHEBI:141969;
ChEMBL	ChEMBL289228 ;
CompTox Dashboard (EPA)	DTXSID5041140 ;
Chemical and physical data
Formula	C27H22Cl2N4O
Molar mass	489.40 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN1C(=O)C=C(c2cccc(Cl)c2)c3cc(ccc13)[C@](N)(c4ccc(Cl)cc4)c5cncn5C;
	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 ; Key:PLHJCIYEEKOWNM-HHHXNRCGSA-N ;
	(what is this?) (verify)

Tipifarnib (INN,^[1]^: 213 proposed trade name Zarnestra) is a farnesyltransferase inhibitor. Farnesyltransferase inhibitors block the activity of the farnesyltransferase enzyme by inhibiting prenylation of the CAAX tail motif, which ultimately prevents Ras from binding to the membrane, rendering it inactive.^[2]

^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 46" (PDF). World Health Organization. Retrieved 16 November 2016.
^ Cox AD, Der CJ, Philips MR (April 2015). "Targeting RAS Membrane Association: Back to the Future for Anti-RAS Drug Discovery?". Clinical Cancer Research. 21 (8): 1819–27. doi:10.1158/1078-0432.CCR-14-3214. PMC 4400837. PMID 25878363.

[INN-1] "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names (Rec. INN): List 46" (PDF). World Health Organization. Retrieved 16 November 2016.

[2] Cox AD, Der CJ, Philips MR (April 2015). "Targeting RAS Membrane Association: Back to the Future for Anti-RAS Drug Discovery?". Clinical Cancer Research. 21 (8): 1819–27. doi:10.1158/1078-0432.CCR-14-3214. PMC 4400837. PMID 25878363.

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