Gamitrinib TPP hexafluorophosphate

Name: Gamitrinib TPP hexafluorophosphate
Brand: MedChemExpress
SKU: HY-102007A
Rating: 5.0 (13 reviews)

Cat. No.: HY-102007A Purity: 99.68%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

CAS No. : 1131626-47-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Gamitrinib TPP hexafluorophosphate:

Gamitrinib TPP Get quote
Gamitrinib TPP hexafluorophosphate (Standard) Get quote

13 Publications Citing Use of MCE Gamitrinib TPP hexafluorophosphate

Cell Imaging/Staining

Cell Proliferation/Viability Assay

Flow Cytometry

: 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.

: 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).

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HSP Isoform Specific Products:

View All Isoforms

HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

HSP90

In Vitro

Gamitrinib TPP (Gamitrinib^TPP, 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.

In Vivo

Whether the combination of TRAIL plus Gamitrinib TPP (Gamitrinib^TPP, G-TPP) has activity against glioblastoma in vivo is studied. Luciferase-expressing U87 glioblastoma cells implanted in the right cerebral striatum of immunocompromised mice give rise to rapidly growing tumors by bioluminescence imaging, and treatment of these mice with vehicle, stereotactic delivery of TRAIL, or systemic administration of suboptimal concentrations of Gamitrinib TPP does not affect tumor growth in vivo. Similarly, systemic monotherapy with Gamitrinib TPP at concentrations (20 mg/kg as daily i.p. injections) that inhibit subcutaneous xenograft tumor growth in mice has no effect on orthotopic glioblastoma growth. In contrast, 2 cycles of intracranial TRAIL combined with systemic Gamitrinib TPP suppresses the growth of established glioblastomas, with no significant animal weight loss throughout treatment^[1].

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

Molecular Weight

1036.03

Formula

C₅₂H₆₅F₆N₃O₈P₂

CAS No.

1131626-47-5

Appearance

Solid

Color

Pale purple to purple

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.9652 mL	4.8261 mL	9.6522 mL
5 mM	0.1930 mL	0.9652 mL	1.9304 mL
10 mM	0.0965 mL	0.4826 mL	0.9652 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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 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.
Protocol 2

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (2.41 mM); Clear solution
Protocol 3

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (2.41 mM); Suspended solution; Need ultrasonic

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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 3.33 mg/mL (3.21 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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).

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.

Purity & Documentation

Purity: 99.68%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (246 KB) HNMR (192 KB) LCMS (102 KB)

Handling Instructions (2659 KB)

References

[1]. Markus D. Siegelin, et al. Exploiting the mitochondrial unfolded protein response for cancer therapy in mice and human cells. J Clin Invest. 2011 Apr 1; 121(4): 1349–1360. [Content Brief]

Cell Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Markus D. Siegelin, et al. Exploiting the mitochondrial unfolded protein response for cancer therapy in mice and human cells. J Clin Invest. 2011 Apr 1; 121(4): 1349–1360. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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