FTI 277 HCl

製品コードS7465 バッチS746504

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₂H₃₀ClN₃O₃S₂

分子量

484.07

CAS No.

180977-34-8

Solubility (25°C)*

体外

DMSO

97 mg/mL (200.38 mM)

Water

97 mg/mL (200.38 mM)

Ethanol (warmed with 50ºC water bath)

97 mg/mL (200.38 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.850mg/ml (10.02mM)
	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.800mg/ml (1.65mM)

* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
in vitro	FTI-277 inhibits Ras processing with an IC50 of 100 nM, but not the geranylgeranylated Rap1A processing in whole cells. This compound 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] It causes increased apoptosis after irradiation and increases radiosensitivity in H-ras-transformed rat embryo cells. ^[2] This chemical also inhibits cell growth and induces apoptosis in drug-resistant myeloma tumor cells. ^[3] In SH-SY5Y cells, this agent 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 HCl (50 mg/kg/d i.p.) effectively clears HDV viremia. ^[5]

プロトコル(参考用のみ)

キナーゼアッセイ	FTase and GGTase I Activity Assay
キナーゼアッセイ	FTI 277 HCl (FTI-277) 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.
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.

参考

https://pubmed.ncbi.nlm.nih.gov/7592920/
https://pubmed.ncbi.nlm.nih.gov/8620483/
https://pubmed.ncbi.nlm.nih.gov/12592346/

https://pubmed.ncbi.nlm.nih.gov/23643986/
https://pubmed.ncbi.nlm.nih.gov/12897208/

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カスタマーフィードバック

: Data from [Data independently produced by , , Cancer Lett, 2018, 442:202-212]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

RHEB neddylation by the UBE2F-SAG axis enhances mTORC1 activity and aggravates liver tumorigenesis [ EMBO J, 2025, 44(4):1185-1219]	PubMed: 39762645
In Vitro synergy of Farnesyltransferase inhibitors in combination with colistin against ESKAPE bacteria [ PLoS One, 2025, 20(9):e0331440]	PubMed: 40911556
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

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。

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