Tipifarnib

ArtNr	S1453-10
Hersteller	Selleckchem
CAS-Nr.	192185-72-1
Menge	10 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 mL 200 mg 50 mg 5 g
Kategorie	Oncology Neuroscience Neuroinflammation Metabolism Diabetes Glucose Homeostasis Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Breast Cancer Heart & Blood Cancer Testicular & Prostate Cancer
Typ	Inhibitors
Specific against	other
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
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	R115777,IND 58359
Similar products	Tipifarnib
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	489, 4
Administration	Oral gavage
Animal Models	Female ovariectomized Ncr foxhead nude mice
Cell lines	MACS-selected CD34+ cells
Clinical Trials	Tipifarnib is currently in phase II clinical trials in previously untreated older adults with AML and baseline presence of a specific 2-gene expression signature ratio.
Concentrations	2.5 nM, 10 nM, 25 nM and 50 nM
Dosages	50 mg/kg
Formulation	20% w/v beta-cyclodextrin (pH 2.5)
IC50	0.6 nM [1], 0.6 nM [1], 0.6 nM [1], 0.6 nM [1], 0.6 nM [1], 0.6 nM [1]
In vitro	Using Tipifarnib 5 uM for 72 hours, the percentage of apoptotic cells is significantly higher in drug-treated compared to DMSO-treated LGL T-cells. Using T-cells from healthy donors, Tipifarnib reduces the percentage of IFNgamma-positive cells in a time-dependent manner. Tipifarnib reduces the amount of activated Ras in precipitates compared to DMSO. [2] Tipifarnib exerts selective in vitro toxicity against clonal MDS hematopoiesis at concentrations less than 10 nM the effect being more prominent in white cell progenitors. This action is not due to apoptosis induction as both normal and MDS progenitors displays equivalent DiOC3 and annexin V expression up to 72 hours after exposure to Tipifarnib. [3] Combining Tipifarnib with 10 nM 4-OH-tamoxifen in the presence of E2 reduces the IC50 8-fold from 400 to 50 nM. [4] Tipifarnib induces apoptosis in U937 cells. [5] In addition, Tipifarnib inhibits isolated human farnesyltransferase for a lamin B peptide and for the K-RasB peptide with IC50 of 0.86 nM and 7.9 nM, respectively. [6]
In vivo	Ki-67 is lower in the tumors treated with E2 withdrawal plus R115777 compared with E2 withdrawal alone. The combination of tamoxifen and R115777 results in significantly lower Ki-67 compared with either tamoxifen or R115777 alone (mean of 5% versus 16.9% and 67.3%, respectively). [4] In contrast, no significant difference in apoptotic scores is seen between the treatment groups. R115777 alone also reduces the CTI compared with control. The combination of tamoxifen and R115777 or R115777 coupled with E2 withdrawal is most effective at lowering the CTI (0.8 and 0.7, respectively), which may account for the decrease in tumor volume. [4]
Incubation Time	48 hours
Method	MACS-selected CD34+ cells are seeded in Methocult 4435 'complete' 1% bovine serum albumin, 3 U/mL recombinant human (rh) erythropoietin, 0.1 mM 2-mercaptoethanol, 2 mM L-glutamine and the following cytokines: 50 ng/mL rh stem cell factor, 20 ng/mL rh GM-CSF, 20 ng/mL rh IL-3, 20 ng/mL rh IL-6 and 20 ng/mL h G-CSF. DMSO or Tipifarnib is added at the concentrations of 2.5, 10, 25 and 50 nM at day 1. All cultures are performed in duplicates and the numbers of colonies are scored after 14 days of incubation at 37 C in a humidified incubator containing 5% CO2.
Solubility (25C)	DMSO 14 mg/mL, Water <1 mg/mL, Ethanol 9 mg/mL
Information	Tipifarnib is a potent and specific farnesyltransferase (FTase) inhibitor with IC50 of 0.6 nM, its anti-proliferative effects are most prominent in H-ras or N-ras mutant cells. Phase 3.
Chemical Name	(R)-6-(amino(4-chlorophenyl)(1-methyl-1H-imidazol-5-yl)methyl)-4-(3-chlorophenyl)-1-methylquinolin-2(1H)-one
Features	Tipifarnib is a potent and selective farnesyl protein transferase inhibitor with significant antitumor effects.

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