Gamitrinib TPP hexafluorophosphate
Based on 16 publication(s) in Google Scholar
Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 99.68%
- CAS No.: 1131626-47-5
- Formula: C52H65F6N3O8P2
- Molecular Weight:1036.03
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Gamitrinib TPP hexafluorophosphate
More- Nature. 2020 Mar;579(7799):433-437. [Abstract]
- Nat Neurosci. 2026 Jun 26. [Abstract]
- Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
- Clin Cancer Res. 2022 May 13;28(10):2180-2195. [Abstract]
- Cancer Lett. 2025 Aug 9:632:217977. [Abstract]
- Cancer Lett. 2022 Nov 28:549:215915. [Abstract]
- Aging Cell. 2026 Jun;25(6):e70573. [Abstract]
- Elife. 2021 Jun 16:10:e63104. [Abstract]
- J Invest Dermatol. 2025 Feb 18:S0022-202X(25)00110-1. [Abstract]
- Am J Physiol Cell Physiol. 2026 Jun 1;330(6):C1721-C1736. [Abstract]
- Front Biosci (Landmark Ed). 2023 Sep 26;28(9):227. [Abstract]
- Exp Ther Med. 2021 Nov;22(5):1246. [Abstract]
- bioRxiv. 2024 September 03.
- bioRxiv. 2024 Jan 2.
- SSRN. 2023 Jul 11.
- Research Square Preprint. 2020 Sep.
Customer Validation & Images
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Cell Imaging/Staining
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Cell Imaging/Staining
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IF
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WB
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Cell Proliferation/Viability Assay
Biological Activity
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HSP90 |
Gamitrinib TPP (GamitrinibTPP, G-TPP), a small molecule that combines the Hsp90 ATPase inhibitory module of 17-allylamino geldanamycin (17-AAG) with the mitochondrial-targeting moiety of triphenylphosphonium. Gamitrinib TPP is selectively delivered to mitochondria and does not affect Hsp90 homeostasis outside the organelle. Within a 16-hour exposure, concentrations of Gamitrinib TPP of 15-20 μM indistinguishably kill patient-derived and cultured glioblastoma cell lines. This cell death response has the hallmarks of mitochondrial apoptosis, with loss of organelle inner membrane potential, release of cytochrome c in the cytosol, activation of initiator caspase-9 and effector caspase-3 and caspase-7, and cellular reactivity for annexin V[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1131626-47-5
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Appearance Solid
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Molecular Weight 1036.03
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Formula C52H65F6N3O8P2
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Color Pale purple to purple
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SMILES
F[P-](F)(F)(F)(F)F.O=C(C=C1NC(/C(C)=C/C=C/[C@H](OC)[C@@H](OC(N)=O)/C(C)=C/[C@H](C)[C@H]2O)=O)C(NCCCCCC[P+](C3=CC=CC=C3)(C4=CC=CC=C4)C5=CC=CC=C5)=C(C[C@H](C[C@@H]2OC)C)C1=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (16)
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Journal Impact Factor
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Most Recent
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Nature
2020 Mar;579(7799):433-437. PMID: 32132706
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Nature. 2020 Mar;579(7799):433-437. [Abstract]
HeLa cells, 293T cells, BJEH fibroblasts and N/TERT-1 keratinocytes were exposed to sgRNAs directed against the specified genes and pharmacologically stimulated for 9-12 h before immunoblotting (one representative experiment shown of n = 2 (HeLa and 293T) or n = 3 (BJEH and N/TERT-1) independent experiments). sgCTR, non-targeting control sgRNA. GTPP, Gamitrinib TPP hexafluorophosphate, HY-102007A, 10 μM.
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Nature. 2020 Mar;579(7799):433-437. [Abstract]
Clonal HAP1 knockout and stably reconstituted cells were treated as indicated (CCCP, 20 μM, 9 h; Tunicamycin, HY-A0098, 10 μM, 9 h; Oligomycin (OM), 9 h; CDDO, Bardoxolone, HY-14909, 2.5 μM, 11 h; GTPP, HY-102007A, 10 μM, 11 h) and analysed by immunoblotting.
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Nature. 2020 Mar;579(7799):433-437. [Abstract]
HAP1 CHOPNeon cells of the indicated genotypes were treated for 9 h (CCCP, 20 μM; Tunicamycin, HY-A0098, 10 μM; CDDO, Bardoxolone, HY-14909, 2.5 μM) or 12 h (GTPP, HY-102007A, 10 μM) and analysed by flow cytometry. Per genotype and treatment, the CHOPNeonsignal was normalized to its DMSO control and statistical significance is indicated compared to identically treated wild-type cells (mean ± s.d. of n = 3 independent experiments; one-way ANOVA with Dunnett’s multiple comparisons correction).
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Nat Neurosci
The mitochondrial unfolded protein response in human microglia disrupts neuronal-glial communication and promotes senescence. [Abstract]2026 Jun 26. PMID: 42362883 -
Sci Adv
In situ characterization of mitochondrial Hsp60-Hsp10 chaperone complex under folding stress. [Abstract]2025 Oct 24;11(43):eadw6064. PMID: 41124257
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Representative immunofluorescence images showing Parkin-eGFP (green) and the mitochondrial marker COXIV (red) in HeLa cells. Cells were treated with dimethyl sulfoxide (DMSO) for 4 hours (h) (top) or GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM) for 4 hours (bottom). Colocalization between Parkin-eGFP and COXIV was assessed using fluorescence intensity profiles. Scale bars, 20 μm.
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Representative tomographic slices (top) and corresponding segmentation images (bottom) of untreated, truncated OTC–expressing, and GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM; for 4 hours)-treated cells. Blue arrowheads indicate electron-dense calcium phosphate granules (untreated), and green arrowheads indicate amorphous aggregates (OTC-expressing and GTPP condition). Scale bars, 50 nm.
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Mitochondrial morphology changes upon stressor treatment. Representative immunofluorescence images of HeLa cells stained for COXIV following treatment with vehicle (CTRL; DMSO), CCCP (4 hours), or GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM; 4 hours). Zoomed-in views highlight mitochondrial network organization under each condition.
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Silver staining analysis of soluble and insoluble protein fractions from siControl and siHsp60/10-treated cells, with or without GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM) treatment. MW, molecular weight.
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Quantification of cellular stress markers following GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM)-induced folding stress under control and knockdown conditions: Cell viability , mitochondrial membrane potential (MitoTracker fluorescence), and mtROS levels. Data are shown as means ± SD. Statistical significance was assessed using unpaired t tests or one-way ANOVA with Tukey’s post hoc test. *P < 0.05; **P < 0.01; ***P < 0.001; ****P < 0.0001.
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Representative immunofluorescence images of HeLa cells under increasing folding stress, comparing siControl (left) and siHsp60/10 knockdown (right) conditions. Cells were treated with DMSO or GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM) for 4 or 8 hours and stained for Parkin-eGFP (green), MitoTracker Red (red), and COXIV (blue). Merged images highlight the mitochondrial network and Parkin puncta localization. Scale bars, 20 μm.
Gamitrinib TPP hexafluorophosphate purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Oct 24;11(43):eadw6064. [Abstract]
Western blot analysis of mitochondrial proteins (TOM20, NDUFS3, Tim23, COXIV, mtHsp60, and mtHsp10) following GTPP (Gamitrinib TPP hexafluorophosphate; 10 μM) treatment for the indicated times. Tubulin was used as a loading control.
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Clin Cancer Res
2022 May 13;28(10):2180-2195. PMID: 35247901 -
Cancer Lett
Restricting metabolic plasticity enhances stress adaptation through the modulation of PDH and HIF1A in TRAP1-depleted colon cancer. [Abstract]2025 Aug 9:632:217977. PMID: 40789509 -
Cancer Lett
Metabolic targeting of NRF2 potentiates the efficacy of the TRAP1 inhibitor G-TPP through reduction of ROS detoxification in colorectal cancer. [Abstract]2022 Nov 28:549:215915. PMID: 36113636 -
Aging Cell
Oxidative Stress and Diminished Mitochondrial Proteostatic Reserve Are Linked to Enhanced mtUPR Initiation in Aged Mouse Muscle. [Abstract]2026 Jun;25(6):e70573. PMID: 42243621 -
Elife
2021 Jun 16:10:e63104. PMID: 34132194 -
J Invest Dermatol
The Differential Roles of HSP90 Isoforms in Skin Inflammation: Anti-Inflammatory Potential of TRAP1 Inhibition. [Abstract]2025 Feb 18:S0022-202X(25)00110-1. PMID: 39978584 -
Am J Physiol Cell Physiol
Divergent mitochondrial stressors elicit specific retrograde signaling pathways in muscle myotubes. [Abstract]2026 Jun 1;330(6):C1721-C1736. PMID: 42126081 -
Front Biosci (Landmark Ed)
Inhibition of TRAP1 Accelerates the DNA Damage Response, Activation of the Heat Shock Response and Metabolic Reprogramming in Colon Cancer Cells. [Abstract]2023 Sep 26;28(9):227. PMID: 37796715 -
Exp Ther Med
2021 Nov;22(5):1246. PMID: 34539842 -
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Solvent & Solubility
DMSO : 50 mg/mL (48.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (2.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 3.33 mg/mL (3.21 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
Human glioblastoma cell lines LN229 (p53 mutant; PTEN, WT), U87 (p53 WT; PTEN mutant), U251 (p53 mutant), prostate adenocarcinoma PC3, breast adenocarcinoma MCF-7, and human epithelial kidney (HEK) 293T are seeded in triplicate onto 96-well plates at 2×103 cells/well, treated with vehicle, Gamitrinib TPP (5, 10, 15, and 20 uM), or nontargeted 17-AAG ( 0-20 μM) for up to 24 h, and quantified for metabolic activity by a MTT colorimetric assay with absorbance at 405 nm. For determination of apoptosis, control or treated tumor cell types (1×106) are labeled for annexin V and propidium iodide (PI) and analyzed by multiparametric flow cytometry. For Gamitrinib TPP-TRAIL combination studies, tumor cell types are simultaneously incubated with suboptimal concentrations of Gamitrinib TPP at 5 μM and TRAIL depending on the cell type at 100 ng/mL (U87), 20 ng/mL (U251), 40 ng/mL (PC3, MCF-7, FHAS), or 200 ng/mL (LN229), and analyzed after 16 h for cell viability by MTT[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
U87 glioblastoma cells stably transfected with a luciferase expression plasmid (U87-Luc) are suspended in sterile PBS, pH 7.2, and stereotactically implanted (1×105) in the right cerebral striatum of immunocompromised nude mice. Animals with established tumors are randomized in 4 groups (4 animals/group) and started on sterile vehicle (cremophor), TRAIL alone, Gamitrinib TPP alone, or the combination of TRAIL plus Gamitrinib TPP. In all animal groups, TRAIL is injected stereotactically in the right cerebral striatum (2 ng on days 7 and 10 after implantation), and Gamitrinib TPP is given systemically (10 mg/kg as daily i.p. injections on days 6, 7, 9, and 10 after implantation). Treatment is suspended on day 10 after tumor implantation, and tumor growth is assessed weekly by bioluminescence imaging after i.p injection of 110 mg/kg D-luciferin. In some experiments, nude mice carrying established U87-Luc intracranial glioblastomas are treated with systemic Gamitrinib TPP monotherapy at 20 mg/kg as daily i.p. injections and monitored for tumor growth by bioluminescence imaging. Animal survival is calculated per group[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 0.9652 mL | 4.8261 mL | 9.6522 mL | 24.1306 mL |
| 5 mM | 0.1930 mL | 0.9652 mL | 1.9304 mL | 4.8261 mL | |
| 10 mM | 0.0965 mL | 0.4826 mL | 0.9652 mL | 2.4131 mL | |
| 15 mM | 0.0643 mL | 0.3217 mL | 0.6435 mL | 1.6087 mL | |
| 20 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2065 mL | |
| 25 mM | 0.0386 mL | 0.1930 mL | 0.3861 mL | 0.9652 mL | |
| 30 mM | 0.0322 mL | 0.1609 mL | 0.3217 mL | 0.8044 mL | |
| 40 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL |
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