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MAPK Raf Lonafarnib

Lonafarnib

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

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

Lonafarnib, CAS 193275-84-2
Pack Size Availability Price/USD Quantity
2 mg In Stock 73.00
5 mg In stock 129.00
10 mg In stock 233.00
25 mg In Stock 420.00
1 mL * 10 mM (in DMSO) In Stock 205.00
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Purity 98.12%
Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
Description Lonafarnib 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 H-ras ,   K-ras-4B ,   N-ras
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)
Cell lines: UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, and UMSCC35, UMSCC38 cell lines
Synonyms Sch66336 , Sarasar , Sch66336 , Sarasar
Purity 98.12%
Molecular Weight 638.82
Formula C27H31Br2ClN4O2
CAS No. 193275-84-2

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 6.4 mg/mL (10 mM)), with gentle warming

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
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

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Anti-infection Compound Library Apoptosis Compound Library Autophagy Compound Library Neuronal Signaling Compound Library MAPK Inhibitor Library Anti-virus Compound Library Immunology/Inflammation Compound Library Kinase Inhibitor Library GPCR Compound Library Anti-cancer Approved drug Library Anti-cancer Clinical Compound Library Anti-cancer Metabolism Compound Library CNS-Penetrant Compound Library Anti-obesity Compound Library Anti-aging Compound Library Anti-cancer Active Compound library Anti-cancer Drug library Drug Repurposing Library HIF-1 Signaling Pathway Compound Library Anti-COVID-19 Compound Library FDA Approved & Pharmacopeial Drug Library Anti-Pancreatic Cancer Compound Library Glutamine Metabolism Compound Library

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