[CAS NO. 193275-84-2] Lonafarnib (SCH66336)

Name: Lonafarnib (SCH66336)
Brand: Arctom Scientific
SKU: SLK-S2797

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PRODUCTS SPECIFICATIONS [193275-84-2]

Store

Catalog

SLK-S2797

Brand

Selleck

CAS

193275-84-2

DESCRIPTION [193275-84-2]

Overview

MDL	MFCD06795138
Molecular Weight	638.82
Molecular Formula	C27H31Br2ClN4O2
SMILES	BrC1=C2[C@](C=3C(CCC2=CC(Cl)=C1)=CC(Br)=CN3)([C@@H]4CCN(C(CC5CCN(C(N)=O)CC5)=O)CC4)[H]

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.5654 mL	7.8269 mL	15.6539 mL
5 mM	0.3131 mL	1.5654 mL	3.1308 mL
10 mM	0.1565 mL	0.7827 mL	1.5654 mL
50 mM	0.0313 mL	0.1565 mL	0.3131 mL

Description

Lonafarnib (SCH66336) is an orally bioavailable FPTase inhibitor for , and with of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.

Targets

H-ras ^[1] (Cell-free assay)	N-ras ^[1] (Cell-free assay)	K-ras-4B ^[1] (Cell-free assay)
1.9 nM	2.8 nM	5.2 nM

In vitro

SCH66336 at concentration ranging from 0.1 μM to 8 μM suppress growth and induce apoptosis of human head and neck squamous carcinoma cells (HNSCC) in a dose and time dependent manner. SCH66336 (8 μM) suppresses protein kinase B/Akt activity as well as the phosphorylation of the Akt substrates glycogen synthase kinase (GSK)-3β, forkhead transcription factor, and BAD in SqCC/Y1 cells. SCH66336 demonstrate variable antiproliferative effects against the cell lines, with IC50 ranging from 0.6 μM to 32.3 μM. 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 μM) activates caspase-8 and its downstream caspases, thus induces caspase-8-dependent apoptosis in H1792 cells. Lonafarnib (5 μM) up-regulate DR5 expression, increase cell-surface DR5 distribution, and enhance tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis in H1792 cells.

In vivo

SCH66336 inhibits HTBI77 human lung carcinoma xenograft growth in nude mice in a dose-dependent fashion. 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.

References

[1] Liu M, et al. Cancer Res, 1998, 58(21), 4947-4956.
[2] Chun KH, et al. Cancer Res, 2003, 63(16), 4796-4800.
[3] Feldkamp MM, et al. Cancer Res, 2001, 61(11), 4425-4431.
[4] Sun SY, et al. J Biol Chem, 2007, 282(26), 18800-18809.

Synonyms

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]-

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]-1-piperidinecarboxamide

Sch 66336

Lonafarnib

Sarasar

Zokinvy