2. Metabolic Enzyme/Protease
  3. Farnesyl Transferase
  4. FGTI-2734

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors.

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FGTI-2734

FGTI-2734 화학구조

CAS No. : 1247018-19-4

사이즈 가격 재고 수량
무료 샘플 (0.1 - 0.2 mg)   지금 신청하기  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 해외재고보유
Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 1 publication(s) in Google Scholar

Other Forms of FGTI-2734:

FGTI-2734 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE FGTI-2734

  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT-1, respectively. FGTI-2734 can prevent membrane localization of KRAS, hence solving KRAS resistance problem and thwarting mutant KRAS patient-derived pancreatic tumors[1].

IC50 & Target

IC50: 250 nM (FT) and 520 nM (GGT-1)[1]
Cellular Effect
Cell Line Type Value Description References
NIH3T3 IC50
0.0887 3
Compound: 21b, FTI-2734
Inhibition of H-Ras farnesylation expressed in mouse NIH3T3 cells
Inhibition of H-Ras farnesylation expressed in mouse NIH3T3 cells
[PMID: 20822181]
NIH3T3 IC50
0.0887 3
Compound: 21b, FTI-2734
Inhibition of H-Ras farnesylation expressed in mouse NIH3T3 cells
Inhibition of H-Ras farnesylation expressed in mouse NIH3T3 cells
[PMID: 20822181]
NIH3T3 IC50
2.7 3
Compound: 21b, FTI-2734
Inhibition of Rap1A geranylgeranylation expressed in mouse NIH3T3 cells
Inhibition of Rap1A geranylgeranylation expressed in mouse NIH3T3 cells
[PMID: 20822181]
NIH3T3 IC50
2.7 3
Compound: 21b, FTI-2734
Inhibition of Rap1A geranylgeranylation expressed in mouse NIH3T3 cells
Inhibition of Rap1A geranylgeranylation expressed in mouse NIH3T3 cells
[PMID: 20822181]
In Vitro

FGTI-2734 (1-30 μM; 72 hours) induces CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells[1].
FGTI-2734 (3-30 μM; 72 hours) inhibits both protein prenylation of HDJ2, RAP1A, KRAS and NRAS. FGTI-2734 inhibits KRAS membrane localization in RAS-transformed murine NIH3T3 cells and in mutant KRAS human cancer cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

FGTI-2734 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MiaPaCa2, L3.6pl and Calu6 cells
Concentration: 1, 3, 10, 30 μM
Incubation Time: 72 hours
Result: Induced CASPASE-3 and PARP cleavage in MiaPaCa2, L3.6pl and Calu6 cells.

Western Blot Analysis[1]

Cell Line: KRAS, HRAS, and NRAS-transformed NIH3T3 cells
Concentration: 3, 10, 30 μM
Incubation Time: 72 hours
Result: Inhibited both protein prenylation of HDJ2, RAP1A, KRAS and NRAS.
In Vivo

FGTI-2734 (intraperitoneally; 100 mg/kg/daily for 18 to 25 days) only inhibits tumor growth in mutant KRAS-dependent tumors but not in mutant KRAS-independent tumors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male SCID-bg mice following injection of MiaPaCa2, L3.6pl, Calu6, A549, H460 and DLD1 cancer cells[1]
Dosage: 100 mg/kg
Administration: Intraperitoneally; daily; for 18 to 25 days
Result: Inhibited tumor growth in mutant KRAS-dependent tumors.
분자량

510.63

화학식

C26H31FN6O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=NC=CC=C1)(N(CCN(C2=CC=C(C#N)C=C2F)CC3=CN=CN3C)CC4CCCCC4)=O
선적

Room temperature in continental US; may vary elsewhere.
보관

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

용액&용해도
In Vitro: 

DMSO : 50 mg/mL (97.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9584 mL 9.7918 mL 19.5837 mL
5 mM 0.3917 mL 1.9584 mL 3.9167 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 몰농도 계산기

  • 농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 7.5 mg/mL (14.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서

Purity: 99.85%

SDS (252 KB)

COA (255 KB) HNMR (213 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9584 mL 9.7918 mL 19.5837 mL 48.9591 mL
5 mM 0.3917 mL 1.9584 mL 3.9167 mL 9.7918 mL
10 mM 0.1958 mL 0.9792 mL 1.9584 mL 4.8959 mL
15 mM 0.1306 mL 0.6528 mL 1.3056 mL 3.2639 mL
20 mM 0.0979 mL 0.4896 mL 0.9792 mL 2.4480 mL
25 mM 0.0783 mL 0.3917 mL 0.7833 mL 1.9584 mL
30 mM 0.0653 mL 0.3264 mL 0.6528 mL 1.6320 mL
40 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2240 mL
50 mM 0.0392 mL 0.1958 mL 0.3917 mL 0.9792 mL
60 mM 0.0326 mL 0.1632 mL 0.3264 mL 0.8160 mL
80 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6120 mL
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FGTI-2734 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

FGTI-27341247018-19-4FGTI2734FGTI 2734Farnesyl TransferaseFtaseC-terminalmimeticfarnesyltransferasegeranylgeranylmembranelocalizationKRASpatient-derivedpancreatictumorsInhibitorinhibitorinhibit

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상품명:
FGTI-2734
Cat. No.:
HY-128350
수량:
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SAFETY DATA SHEET (SDS)

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