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Lonafarnib

Catalog No. T6302   CAS 193275-84-2
Synonyms: Sarasar, Sch66336

Lonafarnib (Sch66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9/5.2/2.8 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Lonafarnib Chemical Structure
Lonafarnib, CAS 193275-84-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
5 mg In stock $ 97.00
10 mg In stock $ 155.00
25 mg In stock $ 313.00
50 mg In stock $ 497.00
100 mg In stock $ 693.00
1 mL * 5 mM (in DMSO) In stock $ 168.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lonafarnib (Sch66336) is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B, and N-ras (IC50: 1.9/5.2/2.8 nM).
Targets&IC50 N-ras:2.8 nM, H-ras:1.9 nM, K-ras-4B: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. [2] SCH66336 demonstrate variable antiproliferative effects against the cell lines, with IC50 ranging from 0.6 μM to 32.3 μM. [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 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.[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]
Kinase Assay FPTactivity is determined by measuring the transfer of [3H]farnesyl from [3H]farnesyl PPi to trichloroacetic acid-precipitable Ha-Ras-CVLS. GGPT-1 activity is similarly determined using [3H]geranylgeranyl diphosphate and Ha-Ras-CVLL as substrates[1].
Cell Research 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) × 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.(Only for Reference)
Synonyms Sarasar, Sch66336
Molecular Weight 638.82
Formula C27H31Br2ClN4O2
CAS No. 193275-84-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL (8.9 mM ), Sonification is recommended

TargetMolReferences and Literature

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. 5. Tangliang Zhao1*, Yi Bao1*,Xinxin Gan1, et al. DNA methylation-regulated QPCT promotes sunitinib resistance by increasing HRAS stability in renal cell carcinoma. Theranostics. 2019, Vol. 9, Issue 21

TargetMolCitations

1. Tangliang Zhao1*, Yi Bao1*,Xinxin Gan1*, Jie Wang1*, Qiong Chen1*, Zhihui Dai2*, Bing Liu 1, Anbang Wang1, Shuhan Sun2, Fu Yang2,3, Linhui Wang1 DNA methylation-regulated QPCT promotes sunitinib resistance by increasing HRAS stability in renal cell carcinoma. Theranostics. 2019, Vol. 9, Issue 21

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Colorectal Cancer Compound Library HIF-1 Signaling Pathway Compound Library Anti-Infection Compound Library CNS-Penetrant Compound Library MAPK Inhibitor Library Reprogramming Compound Library

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Keywords

Lonafarnib 193275-84-2 Autophagy GPCR/G Protein MAPK Metabolism Raf Transferase Ras Inhibitor Sch-66336 Sch 66336 inhibit Farnesyl Transferase Sarasar Ftase Sch66336 inhibitor

 

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