Lonafarnib

Lonafarnibは選択的なファルネシル・タンパク質転移酵素(FPT)阻害剤で、H-ras、 K-ras-4B 、N-ras に作用すると、 IC50 がそれぞれ 1.9 nM、 5.2 nM、2.8 nMになる。

製品コードS2797
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Lonafarnib 化学構造
分子量: 638.82

高品質保証

MSDS

製品説明

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製品の説明

生物活性

製品説明 Lonafarnibは選択的なファルネシル・タンパク質転移酵素(FPT)阻害剤で、H-ras、 K-ras-4B 、N-ras に作用すると、 IC50 がそれぞれ 1.9 nM、 5.2 nM、2.8 nMになる。
ターゲット H-ras K-ras-4B N-ras
IC50 1.9 nM 5.2 nM 2.8 nM [1]
In vitro試験 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試験 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]
臨床試験 SCH66336 has finished phase 2 clinical trial in patients with Metastatic Breast Cancer
特集

プロトコル (参考用のみ)

細胞アッセイ: [2]

細胞株 UMSCC10B, UMSCC14B, UMSCC17B, UMSCC22B, and UMSCC35, UMSCC38 cell lines
濃度 0.1 μM - 8 μM
反応時間 24 hours
実験の流れ 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.

動物実験: [3]

動物モデル NOD/SCID mice between 6–12 weeks of age
製剤 20% (w/v) HPβCD
投薬量 50 mg/kg
投与方法 p.o. bid by oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Lonafarnib SDF
分子量 638.82
化学式

C27H31Br2ClN4O2

CAS No. 193275-84-2
保管 3年-20℃
2年-80℃in solvent
別名 SCH66336
溶解度 (25°C) * In vitro DMSO 127 mg/mL (198.8 mM)
Ethanol 127 mg/mL (198.8 mM)
Water <1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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