FTI-2148 diTFA is aRASC-terminal mimetic dualfarnesyl transferase(FT-1)andgeranylgeranyl transferase-1 (GGT-1)inhibitor withIC₅₀s of 1.4 nM and 1.7 μM, respectively^[1].

IC50: 1.4 nM (FT-1); 1.7 μM (GGT-1)^[1]

FTI-2148 (30 μM) inhibits the farnesylation of the exclusively farnesylated protein HDJ2 in all 3 RAS-transformed NIH3T3 cells^[1].
FTI-2148 diTFA is againstP. falciparumPFT, Mammalian PFT and Mammalian PGGT-I with IC₅₀values of 15 nM; 0.82 nM and 1700 nM, respectively. PFT:protein farnesyltransferase; PGGT-I geranylgeranyltransferase-I^[2].

FTI-2148 (intraperitoneal injection; 25 or 50 mpk/day with a mini-pump; started on day 15 and stopped on day 45 and restarted day 53-83) inhibits the tumor growth by 91% in human lung adenocarcinoma A-549 cells induced mouse model^[1].
FTI-2148 (subcutaneous injection; 25 mpk/day with a mini-pump; 14 days) inhibits tumor growth by 77%by the end of the 2-week treatment in Human Xenograft Nude Mouse Model^[1].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 14 days) results in breast tumor regression in a ras transgenic mouse model^[3].
FTI-2148 (subcutaneous injection; 100 mg/kg/day; 4 days) results in 85–88% inhibition of FTase with no inhibition of GGTase I enzymatic activity in breast tumors from mice in vivo settings^[3].

680.62

C₂₈H₃₀F₆N₄O₇S

817586-01-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

Ethanol : 5 mg/mL(7.35 mM;Need ultrasonic)

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% EtOH40%PEG3005%Tween-8045% saline

  Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

  此方案可获得 ≥ 0.5 mg/mL (0.73 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% EtOH90% (20%SBE-β-CDin saline)

  Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

  此方案可获得 ≥ 0.5 mg/mL (0.73 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 EtOH 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% EtOH90%corn oil

  Solubility: ≥ 0.5 mg/mL (0.73 mM); Clear solution

  此方案可获得 ≥ 0.5 mg/mL (0.73 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中，混合均匀。