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GGTI-2418 

Cat. No.: HY-16231 Purity: 99.27%
Handling Instructions

GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors.

For research use only. We do not sell to patients.

GGTI-2418 Chemical Structure

GGTI-2418 Chemical Structure

CAS No. : 501010-06-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors[1].

IC50 & Target

IC50: 9.5 nM (GGTase I), 53 μM (FTase)[1]

In Vitro

GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5±2.0 nM and 53±11 μM, respectively, a 5,600-fold selectivity toward inhibition of GGTase I versus FTase. GGTI-2418 demonstrates competitive inhibition of GGTase I against the H-Ras-CVLL protein with a Ki of 4.4±1.6 nM[1].
GGTi-2418 (10-15 μM; 16 hours) treatment delocalizes FBXL2 and stabilizes IP3R3[2].

Western Blot Analysis[2]

Cell Line: HeLa cells
Concentration: 10-15 μM
Incubation Time: 16 hours
Result: Delocalized FBXL2 and stabilized IP3R3.
In Vivo

GGTI-2418 (100 mg/kg daily or 200 mg/kg every third day; 15 days) significantly inhibits the growth of breast tumor xenografts in nude mice with MDA-MB-231 xenografts[1].
GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice[1].
GGTI-2418 inhibits the geranylgeranylation of Rap1 and causes a dramatic decrease in S473 phosphorylation of Akt. GGTI-2418 also upregulates p27 levels in vivo[1].

Animal Model: Nude mice implanted with MDA-MB-231 breast cancer tumors[1]
Dosage: 100 mg/kg daily or 200 mg/kg every third day
Administration: Injected intraperitoneally; 15 days
Result: Inhibited the growth of breast tumor xenografts.
Animal Model: ErbB2 transgenic mice[1]
Dosage: 100 mg/kg/day
Administration: Subcutaneously; 5 days
Result: Halted tumor growth and induced massive tumor regression. Tumor decreased by 76% following GGTI-2418 treatment.
Clinical Trial
Molecular Weight

441.52

Formula

C₂₃H₃₁N₅O₄

CAS No.

501010-06-6

SMILES

CC(C)C[[email protected]@H](C(O)=O)NC(N1[[email protected]@H](CC2=CC=CC=C2)C(N(CC3=C(C)N=CN3)CC1)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (283.11 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2649 mL 11.3245 mL 22.6490 mL
5 mM 0.4530 mL 2.2649 mL 4.5298 mL
10 mM 0.2265 mL 1.1325 mL 2.2649 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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GGTI-2418
Cat. No.:
HY-16231
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