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Lonafarnib (SCH66336)

Lonafarnib (SCH66336)

ArtNr	S2797-10000
Hersteller	Selleckchem
CAS-Nr.	193275-84-2
Menge	10 g
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 200 mg 25 mg 5 mg 5 g
Kategorie	Oncology Metabolism Cholesterol & Lipid Metabolism Enzymes Other Fatty Acid Enzymes Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Skin Cancer Breast Cancer
Typ	Inhibitors
Specific against	other
Smiles	C1CN(CCC1CC(=O)N2CCC(CC2)C3C4=C(CCC5=C3N=CC(=C5)Br)C=C(C=C4Br)Cl)C(=O)N
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	H-ras,K-ras-4B,N-ras,Transferase
Similar products	Lonafarnib
Lieferbar
Storage Conditions	2 years -80 in solvent
Molecular Weight	638, 82
Administration	p.o. bid by oral gavage
Animal Models	NOD/SCID mice between 6â€“12 weeks of age
Cell lines	UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, and UMSCC35, UMSCC38 cell lines
Clinical Trials	SCH66336 has finished phase 2 clinical trial in patients with Metastatic Breast Cancer
Concentrations	0.1 uM - 8 uM
Dosages	50 mg/kg
Formulation	20% (w/v) HPbetaCD
IC50	1.9 nM, 1.9 nM, 1.9 nM, 1.9 nM, 1.9 nM, 1.9 nM
In vitro	SCH66336 at concentration ranging from 0.1 uM to 8 uM suppress growth and induce apoptosis of human head and neck squamous carcinoma cells (HNSCC) in a dose and time dependent manner. SCH66336 (8 uM) suppresses protein kinase B/Akt activity as well as the phosphorylation of the Akt substrates glycogen synthase kinase (GSK)-3beta, forkhead transcription factor, and BAD in SqCC/Y1 cells. [2] SCH66336 demonstrate variable antiproliferative effects against the cell lines, with IC50 ranging from 0.6 uM to 32.3 uM. [3] Lonafarnib induces a CCAAT/enhancer-binding protein homologous protein (CHOP)-dependent transactivation of the DR5 promoter, thus induces CHOP-dependent DR5 up-regulation. Lonafarnib (< 10 uM) activates caspase-8 and its downstream caspases, thus induces caspase-8-dependent apoptosis in H1792 cells. Lonafarnib (5 uM) up-regulate DR5 expression, increase cell-surface DR5 distribution, and enhance tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis in H1792 cells.[4]
In vivo	SCH66336 inhibits HTBI77 human lung carcinoma xenograft growth in nude mice in a dose-dependent fashion. [1] SCH66336 dosed at 50 mg/kg p.o. bid by oral gavage inhibits tumor growth with up to 69% growth inhibition after 21 days of treatment in NOD/SCID mice bearing s.c. flank XEN01, XEN05 or XEN08 GBM xenografts. [3]
Incubation Time	24 hours
Method	The cells are seeded in 96-well cell-culture cluster plates at a density that allowed control cultures to grow exponentially for 5 days. After 24 hours, the cells are treated with different concentrations of SCH66336. SCH66336 is dissolved in DMSO. Control cultures received the same amount of DMSO as the treated cultures do. Cell numbers are estimated after 5 days of treatment by SRB assay. The percentage of growth inhibition is calculated by using the equation: percentage growth inhibition = (1 At/Ac) x 100, where At and Ac represent the absorbance in treated and control cultures, respectively. The drug concentration causing a 50% cell growth inhibition (IC50), is determined by interpolation from dose-response curves.
Solubility (25C)	DMSO 127 mg/mL, Water <1 mg/mL, Ethanol 127 mg/mL
Information	Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.
Chemical Name	1-Piperidinecarboxamide, 4-[2-[4-[(11R)-3, 10-dibromo-8-chloro-6, 11-dihydro-5H-benzo[5, 6]cyclohepta[1, 2-b]pyridin-11-yl]-1-piperidinyl]-2-oxoethyl]-

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S2797-10000-datasheet.pdf

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