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ChemicalBook > Product Catalogue >Biochemical Engineering >Inhibitors >Metabolism >Transferase Inhibitors >LONAFARNIB

LONAFARNIB

LONAFARNIB Structure
  • ₹13531.25 - ₹54428.1
  • Product name: LONAFARNIB
  • CAS: 193275-84-2
  • MF: C27H31Br2ClN4O2
  • MW: 638.82
  • EINECS:
  • MDL Number:MFCD06795138
  • Synonyms:LONAFARNIB;4-(2-(4-((R)-3,10-dibroMo-8-chloro-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)cyclohexyl)-2-oxoethyl)piperidine-1-carboxaMide;Lonafarnib (SCH66336);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-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo-(5,6)-cyclohepta(1,2-B)-pyridin-11(R)-yl)-1-piperidinyl)-2-oxo-ethyl)-1-piperidinecarboxamide;Lonafarnib [usan];Sarasar;Sch 66336
2 prices
Selected condition:

Brand

  • Sigma-Aldrich(India)

Package

  • 5MG
  • 25MG
  • ManufacturerSigma-Aldrich(India)
  • Product numberSML1457
  • Product descriptionLonafarnib ≥98% (HPLC)
  • Packaging5MG
  • Price₹13531.25
  • Updated2022-06-14
  • Buy
  • ManufacturerSigma-Aldrich(India)
  • Product numberSML1457
  • Product descriptionLonafarnib ≥98% (HPLC)
  • Packaging25MG
  • Price₹54428.1
  • Updated2022-06-14
  • Buy
Manufacturer Product number Product description Packaging Price Updated Buy
Sigma-Aldrich(India) SML1457 Lonafarnib ≥98% (HPLC) 5MG ₹13531.25 2022-06-14 Buy
Sigma-Aldrich(India) SML1457 Lonafarnib ≥98% (HPLC) 25MG ₹54428.1 2022-06-14 Buy

Properties

Melting point :214.5-215.9° (monohydrate); mp 222-223°
alpha :D25 = +49.1° (c = 0.21 in methanol)
Boiling point :710.4±70.0 °C(Predicted)
Density :1.536
storage temp. :-20°C
solubility :Chloroform (Slightly), Methanol (Slightly)
pka :15.76±0.40(Predicted)
form :powder
color :white to beige

Safety Information

Symbol(GHS): GHS hazard pictograms
Signal word: Warning
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H315 Causes skin irritation Skin corrosion/irritation Category 2 Warning GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 Causes serious eye irritation Serious eye damage/eye irritation Category 2A Warning GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 May cause respiratory irritation Specific target organ toxicity, single exposure;Respiratory tract irritation Category 3 Warning GHS hazard pictograms
Precautionary statements:
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P264 Wash hands thoroughly after handling.
P264 Wash skin thouroughly after handling.
P271 Use only outdoors or in a well-ventilated area.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352 IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338 IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Description

Farnesyl transferase drives the post-translational farnesylation of a number of target proteins, including Ras, a component of the MAPK and Akt signaling pathways involved in cell proliferation, and Ras homolog enriched in brain (Rheb), which stimulates mTOR activity. By arresting growth, farnesyl transferase inhibitors have great potential as antitumor agents. Lonafarnib is a farnesyl transferase inhibitor that blocks the post-translational lipid modification of oncogenic Ras isoforms H-Ras, N-Ras, and K-Ras (IC50s = 1.9, 2.8, and 5.2 nM, respectively) as well as Rheb (IC50 = 10-100 nM). It inhibits H-Ras signaling in whole cells (IC50 = 10 nM) and blocks the transformed growth properties of fibroblasts (IC50 = 75 nM) and human tumor cell lines (IC50 = 400 nM) expressing activated K-Ras proteins. In the nude mouse, lonafarnib demonstrates potent dose-dependent oral activity in an array of human tumor xenograft models including tumors originating from colon, lung, pancreas, prostate, and urinary bladder. Combination treatments with various cytotoxic agents (cyclophosphamide, 5-fluorouracil, and vincristine) or MAPK or Akt pathway inhibitors can enhance the in vivo efficacy of lonafarib.

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