受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C22H30ClN3O3S2 |
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分子量 | 484.07 | CAS No. | 180977-34-8 | |
Solubility (25°C)* | 体外 | DMSO | 96 mg/mL (198.31 mM) | |
Water | 96 mg/mL (198.31 mM) | |||
Ethanol | 14 mg/mL warmed with 50ºC water bath (28.92 mM) | |||
* <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. |
製品説明 | FTI 277 HCl is a potent and selective farnesyltransferase (FTase) inhibitor with IC50 of 500 pM, about 100-fold selectivity over the closely related GGTase I. FTI 277 HCl inhibits cell growth and induces apoptosis. FTI 277 HCl is effective in clearing HDV viremia. |
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in vitro | FTI-277 inhibits Ras processing with an IC50 of 100 nM, but not the geranylgeranylated Rap1A processing in whole cells. FTI-277 induces accumulation of cytoplasmic non-farnesylated H-Ras, accumulates inactive Ras/Raf complexes in the cytoplasm, and blocks constitutive MAPK activation in H-RasF cells. [1] FTI-277 causes increased apoptosis after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells. [2] FTI-277 also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells. [3] In SH-SY5Y cells, FTI-277 diminishes the toxic effects of methamphetamine on induction in cell degeneration, activation in c-Jun-N-terminal kinase cascades, and Ras activation. [4] |
in vivo | In mice coinfected with hepatitis B virus (HBV) and HDV, FTI-277 (50 mg/kg/d i.p.) effectively clears HDV viremia. [5] |
キナーゼアッセイ | FTase and GGTase I Activity Assay | |
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FTase and GGTase I activities from 60,000×g supernatants of human Burkitt lymphoma (Daudi) cells are assayed. Inhibition studies are performed by determining the ability of Ras CAAX peptidomimetics to inhibit the transfer of [3H]farnesyl and [3H]geranylgeranyl from [3H]farnesylpyrophosphate and [3H]geranylgeranylpyrophosphate to H-Ras-CVLS and H-Ras-CVLL, respectively. | ||
細胞アッセイ | 細胞株 | 8226, U266, and H929 multiple myeloma cell lines |
濃度 | ~10 μM | |
反応時間 | 96 hours | |
実験の流れ | Cells are seeded at 8000–14 000 cells/well in 96-well plates. To establish a dose–response to FTI-277, cells are incubated for 96 h in two-fold serial dilutions ranging from 3.75 times 10-7 M to 1 times 10-5 M. Following continuous drug exposure, 50 μL MTT dye is added. The insoluble formazan complex is solubilized with DMSO and absorbance measured at 540 nm. IC50s and 95% confidence intervals are calculated by regression analysis of the linear portion of the dose–response curve. |
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動物実験 | 動物モデル | HBV/HDV-transgenic FVB mice |
投薬量 | 50 mg/kg/d | |
投与方法 | i.p. |
Data from [Data independently produced by , , Cancer Lett, 2018, 442:202-212]
Caffeine Supplementation and FOXM1 Inhibition Enhance the Antitumor Effect of Statins in Neuroblastoma [ Cancer Res, 2023, 83(13):2248-2261] | PubMed: 37057874 |
Farnesyl pyrophosphate is a new danger signal inducing acute cell death [ PLoS Biol, 2021, 19(4):e3001134] | PubMed: 33901180 |
Mevalonate Pathway-mediated ER Homeostasis Is Required for Haploid Stability in Human Somatic Cells [ Cell Struct Funct, 2021, 46(1):1-9] | PubMed: 33361684 |
Cellular basis underlying the intolerance to haploidy in vertebrates [ HOKKAIDO UNIVERSITY, 2021, 10.14943/doctoral.k14392] | PubMed: None |
LUBAC controls chromosome alignment by targeting CENP-E to attached kinetochores [ Nat Commun, 2019, 10(1):273] | PubMed: 30655516 |
FBXW7 regulates endothelial barrier function by suppression of the cholesterol synthesis pathway and prenylation of RhoB [ Mol Biol Cell, 2019, 30(5):607-621] | PubMed: 30601691 |
Zoledronic acid enhances the efficacy of the MEK inhibitor trametinib in KRAS mutant cancers [Dai X, et al. Cancer Lett, 2018, 442:202-212] | PubMed: 30429107 |
Inhibition of YAP reverses primary resistance to EGFR inhibitors in colorectal cancer cells. [ Oncol Rep, 2018, 40(4):2171-2182] | PubMed: 30106444 |
Inhibition of YAP reverses primary resistance to EGFR inhibitors in colorectal cancer cells [ Oncol Rep, 2018, 40(4):2171-2182] | PubMed: 30106444 |
Palmitoylated SCP1 is targeted to the plasma membrane and negatively regulates angiogenesis [ Elife, 2017, 6e22058] | PubMed: 28440748 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。