Tipifarnib Inhibitor CAS No. 192185-72-1

Cat. No.	Name	Size	Price
KI0142	Tipifarnib	10 mg	$768
	Tipifarnib	50 mg	$1568
	Tipifarnib	200 mg	$3808

Chemical Characteristic

Product Name	Tipifarnib
Synonyms	R115777, Zarnestra
CAS No.	192185-72-1
Molecular Weight	489.4
Formula	C₂₇H₂₂Cl₂N₄O
Chemical Name	(R)-6-(amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one
Smiles	n1(c(=O)cc(c2cc(ccc12)[C@@](c1cncn1C)(c1ccc(cc1)Cl)N)c1cc(ccc1)Cl)C
Chemical Structure

Biological activities

Tipifarnib is a newly synthesized potent farnesyl transferase inhibitor (FTI) which exerts biologic effect via potent and selective targeting of protein farnesyl transferase (FTase), resulting in modulation of the tumor protein activity and disruption of multiple cell-signaling pathways. Tipifarnib competitively inhibits the farnesylation of lamin B and K-Ras B peptide substrates, with IC50s of 0.86 and 7.9 nM, respectively. In a panel of human tumor cell lines (including T24F1, CAPAN-2 cells) tested for growth inhibition, more than 75% are found to be sensitive to tipifarnib, and the majority of sensitive cell lines have a wild-type ras gene. ^[1] Tipifarnib demonstrates significant activity in hematologic disorders, including acute myeloid leukemia (AML), multiple myeloma (MM), myelodysplastic syndrome (MDS), and chronic myelogenous leukemia (CML), with complete response rates in AML and MDS of up to approximately 15%. Tipifarnib inhibits AML colony-forming unit leukemia (CFU-L) and normal granulocyte-macro-phage progenitors (CFU-GM) cells with IC50s of 67.1 and 121.9 nM, respectively. Besides, tipifarnib at the concentrations from 10 to 100 nM is able to inhibit growth of cell lines such as HL60 and AML blasts. ^[2] In human breast cancer cell lines in vitro, tipifarnib inhibits BT-474 and MDA-MB-231 with IC50s of 5.4 and 28.9 µM. And the combination of tipifarnib plus paclitaxel inhibits the production of pro-angiogenic growth factors in HER2/neu low and overexpressing breast cancer cells greatly.^[3] Meanwhile, tipifarnib inhibits the growth of human myeloma cell lines U266 and NCI-H929 dose-dependently at concentrations ranging from 10 nM to 1.0 µM, but inhibits weakly the growth of RPMI8226 cells. In the U266 cell line, tipifarnib at 10 nM induces apoptosis time-dependently and the percentage of late apoptotic and necrotic cells increases gradually.^[4] Oral administration b.i.d. of tipifarnib to nude mice bearing s.c. tumors at doses ranging from 6.25??00 mg/kg inhibits the growth of tumors bearing mutant H-ras, mutant K-ras, and wild-type ras genes.^[1]

Protocols

Tipifarnib is diluted in DMSO. ^[1]

References

[1] End DW, et al. Characterization of the antitumor effects of the selective farnesyl protein transferase inhibitor R115777 in vivo and in vitro. Cancer Res. 2001, 61(1): 131-137. [2] Korycka A, et al. The influence of farnesyl protein transferase inhibitor R115777 (Zarnestra) alone and in combination with purine nucleoside analogs on acute myeloid leukemia progenitors in vitro. Eur J Haematol. 2004, 73(6): 418-426. [3] Izbicka E, et al. Biomarkers of anticancer activity of R115777 (Tipifarnib, Zarnestra) in human breast cancer models in vitro. Anticancer Res. 2005, 25(5): 3215-3223. [4] Ochiai N, et al. Effect of farnesyl transferase inhibitor R115777 on the growth of fresh and cloned myeloma cells in vitro. Blood. 2003, 102(9): 3349-3353.

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