GGTI298 |
Catalog No.GC36134
One-Click Copy Product Info
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GGTI298 is a selective, irreversible inhibitor of geranylgeranyltransferase I (GGTase-I) (IC50 = 3μM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 180977-44-0
Sample solution is provided at 25 µL, 10mM.
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GGTI298 is a selective, irreversible inhibitor of geranylgeranyl transferase I (GGTase-I) (IC50 = 3μM) [1]. By inhibiting GGTase-I, GGTI298 blocks geranylgeranylation of small GTPases such as RhoA, leading to cell cycle arrest at the G0/G1 phase and induction of apoptosis [2-3]. GGTI298 is primarily used to treat non-small cell lung cancer [4].
In A549 cells, Gefitinib and GGTI298 (2.5-5µM; 48h) have synergistic anti-proliferative effects on cells [5]. In A549 cells, GGTI298 (15µM; 48h) induces cell apoptosis [6].
In Luc-G33 cells xenograft mice model, combination treatment with Zoledronate and GGTI298 (1.16mg/kg; sc; 35d) both reduced tumor growth [7].
References:
[1]. Dan H C, Jiang K, Coppola D, et al. GGTI 298[J]. Oncogene, 2004, 23: 706-715.
[2]. Peterson Y K, Kelly P, Weinbaum C A, et al. A novel protein geranylgeranyltransferase-I inhibitor with high potency, selectivity, and cellular activity[J]. Journal of Biological Chemistry, 2006, 281(18): 12445-12450.
[3]. Vogt A, Sun J, Qian Y, et al. The geranylgeranyltransferase-I inhibitor GGTI-298 arrests human tumor cells in G0/G1 and induces p21WAF1/CIP1/SDI1 in a p53-independent manner[J]. Journal of Biological Chemistry, 1997, 272(43): 27224-27229.
[4]. Chen S, Fu L, Raja S M, et al. Dissecting the roles of DR4, DR5 and c-FLIP in the regulation of geranylgeranyltransferase I inhibition-mediated augmentation of TRAIL-induced apoptosis[J]. Molecular cancer, 2010, 9(1): 23.
[5]. Liu B S, Dai X Y, Xia H W, et al. Geranylgeranyl transferase 1 inhibitor GGTI-298 enhances the anticancer effect of gefitinib[J]. Molecular Medicine Reports, 2018, 18(4): 4023-4029.
[6]. Miquel K, Pradines A, Sun J, et al. GGTI-298 induces G0-G1 block and apoptosis whereas FTI-277 causes G2-M enrichment in A549 cells[J]. Cancer research, 1997, 57(10): 1846-1850.
[7]. Lau C P Y, Wong K C, Huang L, et al. A mouse model of luciferase-transfected stromal cells of giant cell tumor of bone[J]. Connective tissue research, 2015, 56(6): 493-503.
| Cell experiment [1]: | |
Cell lines | A549 cells |
Preparation Method | A549 cells were seeded (5×103 cells per well in 100µL DMEM with 10% FBS) in a 96-well flat-bottomed plate at 24h prior to treatment. A549 cells were treated with gefitinib (5µM) and/or GGTI298 (concentration indicated) for 48h at 37℃ in a humidified (5% CO2, 95% air) incubator. Following incubation at 37℃, cell growth was measured using a Cell Counting Kit-8. |
Reaction Conditions | 2.5-5µM; 48h |
Applications | Gefitinib and GGTI298 have synergistic anti-proliferative effects on cells. |
| Animal experiment [2]: | |
Animal models | Luc-G33 cells xenograft mice model |
Preparation Method | The nude mice were initially weighed and anesthetized intraperitoneally with 10% chloral hydrate at 0.1ml/30g live weight. The operative area was prepared with iodine. Each mouse was then given an intraosseous (1×106) and a subcutaneous injection (3×106) of Luc-G33 cells in hydrogel into the tibia and under the dorsal skin, respectively. A preliminary study had been proceeded on eight mice for observing the duration of the BLI signals from the Luc-G33 cells in the mice in vivo. Thirty-two mice after Luc-G33 implantation were randomly divided into four groups (8 mice/group) with equal average body weight and drugs were given to each mice three days after cell injection. Group 1 was then given 0.9% sodium chloride (Abbott) as the vehicle control treatment; Groups 2–4 were given Zoledronate (ZOL) and GGTI298 treatments at the following dosages: group 2 treated with ZOL alone at 400mg/kg; group 3 with GGTI298 alone at 1.16mg/kg; and group 4 with the combination of ZOL at 400mg/kg and GGTI298 at 1.16mg/kg. |
Dosage form | 1.16mg/kg; sc; 35d |
Applications | Combination treatment with Zoledronate and GGTI298 both reduced tumor proliferation. |
References: | |
| Cas No. | 180977-44-0 | SDF | |
| Canonical SMILES | CC(C)C[C@@H](C(OC)=O)NC(C1=CC=C(NC[C@@H](N)CS)C=C1C2=C3C=CC=CC3=CC=C2)=O | ||
| Formula | C27H33N3O3S | M.Wt | 479.63 |
| Solubility | DMSO: 100 mg/mL (208.49 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0849 mL | 10.4247 mL | 20.8494 mL |
| 5 mM | 417 μL | 2.0849 mL | 4.1699 mL |
| 10 mM | 208.5 μL | 1.0425 mL | 2.0849 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)