Home > Signaling Pathways>Apoptosis>Apoptosis>GGTI-2418
GGTI-2418

This product is for research use only, not for human use. We do not sell to patients.

GGTI-2418
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
100mg$2915To Be Confirmed
200mg$4370To Be Confirmed
500mg$7375To Be Confirmed
email: [email protected]        [email protected]

Cat #: V21574 CAS #: 501010-06-6 Purity ≥ 99%

Description: GGTI-2418 (GGTI2418; GGTI 2418; PTX-100; PTX100) is a novel, potent and peptidomimetic inhibitor of geranylgeranyltransferase I (GGTase I) with anticancer activity.

References: Kazi A, et al. Blockade of protein geranylgeranylation inhibits Cdk2-dependent p27Kip1 phosphorylation on Thr187 and accumulates p27Kip1 in the nucleus: implications for breast cancer therapy. Mol Cell Biol. 2009 Apr;29(8):2254-63.

Top Publications Citing Invivochem Products
Product Catalog 2022
Bulletin Board
Guide to Product Handling
Publications Citing InvivoChem Products
Product Promise
Promise
Molecular Weight (MW)441.52
Molecular FormulaC23H31N5O4
CAS No.501010-06-6
SMILES CodeCC(C)C[C@H](NC(N1[C@@H](CC2=CC=CC=C2)C(N(CC3=C(C)N=CN3)CC1)=O)=O)C(O)=O
SynonymsPTX-100; PTX 100; PTX100; : GGTI2418; GGTI-2418; GGTI 2418;
ProtocolIn VitroGGTI-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.
In VivoGGTI-2418 inhibits the geranylgeranylation of Rap1 and causes a dramatic decrease in S473 phosphorylation of Akt. GGTI-2418 also upregulates p27 levels in vivo. GGTI-2418 (100 mg/kg daily; 5 days) induces regression of ErbB2-driven mammary tumors in ErbB2 transgenic mice. 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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM2.2649 mL11.3245 mL22.6490 mL45.2981 mL
5mM0.4530 mL2.2649 mL4.5298 mL9.0596 mL
10mM0.2265 mL1.1325 mL2.2649 mL4.5298 mL
20mM0.1132 mL0.5662 mL1.1325 mL2.2649 mL
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
 
=
Concentration
 
×
Volume
 
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
 
×
 
Volume(start)
V1
 
=
 
Concentration(final)
C2
 
×
 
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O
Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.