Lonafarnib

製品コードS2797 別名:SCH66336

Lonafarnib化学構造

分子量(MW):638.82

Lonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.

サイズ 価格(税別)  
JPY 71380.00
JPY 28220.00
JPY 44820.00

カスタマーフィードバック(2)

  • Huh-7/hNTCP cells were infected with in vitro generated HDV in the presence or absence of MyrB (50 nM) or lonafarnib (200 nM). After 5 days cells were labeled with HDAg#280, secondary AF488 and stained with DAPI. A representative of four independent experiments is shown.

    Antiviral Res, 2017, 141:116-123. Lonafarnib purchased from Selleck.

    Low-dose lonafarnib decreased HIF-1α expression without inhibiting cell growth in MDA-MB-231 cells. (A, B) Lonafarnib (1 μM) treatment for 24 h significantly decreased HIF-1α expression, which was normalized to that of GAPDH. In contrast, lonafarnib (1 μM) did not decrease HIF-2α expression.

    J Cell Physiol, 2017, 232(1):192-201. Lonafarnib purchased from Selleck.

製品安全説明書

Transferase阻害剤の選択性比較

生物活性

製品説明 Lonafarnib is an orally bioavailable FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM in cell-free assays, respectively. Phase 3.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Cos-1 monkey kidney cells MXHGeY5kfGmxbjDhd5NigQ>? MWTJcohq[mm2aX;uJI9nKFC{b4TlbY4h\mG{bnXzfYx1emGwc3\ldoF{\SCrbjDDc5MuOSCvb37r[Zkhc2mmbnX5JINmdGy|IHX4dJJme3OrbnegTE1T[XNvdnHsMEBKSzVyPUCuNFAyQSEQvF2= M{\wS|EzOTlyM{C5
COS-7 monkey cells NIC1R3ZHfW6ldHnvckBie3OjeR?= MmG5TY5pcWKrdHnu[{B1cGViZnHycoV{gWyjdHnvckBw\iCKLYLhd{Bxem:2ZXnud{BqdiCFT2OtO{Bud26tZYmgZ4VtdHNidILhcpNq\W62bImg[ZhxemW|c3nu[{BJNXKjc2vWZYwyOl1vQ2\MV{BqdiC2aHWge4hwdGViY3XscEBie3OjeTygTWM2OD1yLkCxJO69VQ>? M1LNXFk5OjJ3NUi=
MCF-7 tumor cell line M1XTbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MojuR49ueG:3bnSge4F{KG2nYYP1doVlKG[xcjDpcohq[mm2aX;uJI9nKE2FRj23JJR2dW:{IHPlcIwhdGmwZTDpckBjemWjc4SgeY5l\XJic3;meEBi\2G{IHHzd4F6NCCLQ{WwQVAvODVizszN NFzPfWw6QDJ{NUW4
HCT116 NX3XOYRbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlvCR49ueG:3bnSge4F{KG2nYYP1doVlKG[xcjDpcohq[mm2aX;uJI9nKEiFVEGxOkB1fW2xcjDj[YxtKGyrbnWgbY4h[2:ub36geY5l\XJic3;meEBi\2G{IHHzd4F6NCCLQ{WwQVAvODdizszN NFHMdnI6QDJ{NUW4
NIH-H tumor cell lines MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFzWe|REd22yb4Xu[EBi[mmuaYT5JJRwKGmwaHnibZQh[W6laH;yZYdmNWmwZHXw[Y5l\W62IHfyc5d1cCCxZjDOTWguUCC2dX3vdkBk\WyuIHzpcoV{KGmwIIPv[pQh[WejcjygTWM2OD1yLkC3NkDPxE1? M3;QXVk5OjJ3NUi=
NIH3T3 cells MkLoSpVv[3Srb36gZZN{[Xl? NFXjZpdKdmirYnn0bY9vKG:oIGLhd{Bn[XKwZYP5cIF1cW:wIHnuJGguWmG|IITyZY5{\m:{bXXkJG5KUDOWMzDj[YxteyxiRVO1NF0xNjFizszN NGnWVmsyPTR3NEKyPC=>
NIH-K tumor cell lines M2\seGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPJRZRIS2:vcH;1coQh[WKrbHn0fUB1dyCrbnjpZol1KGGwY3jvdoFo\S2rbnTldIVv\GWwdDDndo94fGhib3[gUmlJNUtidIXtc5Ih[2WubDDsbY5meyCrbjDzc4Z1KGGpYYKsJGlEPTB;MD61JO69VQ>? M1jWOVk5OjJ3NUi=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験: [2]
+ 展開
  • 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.
    (参考用のみ)
動物試験:[3]
+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 127 mg/mL (198.8 mM)
Ethanol 127 mg/mL (198.8 mM)
Water Insoluble

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 638.82
化学式

C27H31Br2ClN4O2

CAS No. 193275-84-2
保管
in solvent
別名 SCH66336

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02511431 Completed Hepatitis D National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|National Institutes of Health Clinical Center (CC) July 29 2015 Phase 2
NCT02968641 Not yet recruiting Chronic Delta Hepatitis Eiger BioPharmaceuticals March 2017 Phase 2
NCT02579044 Recruiting Progeria Boston Children’s Hospital December 2015 Phase 1|Phase 2
NCT02527707 Completed Chronic Delta Hepatitis Eiger BioPharmaceuticals|Hannover Medical School September 2015 Phase 2
NCT02430194 Completed Chronic Hepatitis D Infection Eiger BioPharmaceuticals|Ankara University December 2014 Phase 2
NCT02430181 Completed Chronic Hepatitis D Infection Eiger BioPharmaceuticals November 2014 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

Transferaseシグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID