1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease
  2. HSP
  3. Gamitrinib TPP hexafluorophosphate

Gamitrinib TPP hexafluorophosphate 

Cat. No.: HY-102007A Purity: 98.52%
COA Handling Instructions

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.

Gamitrinib TPP hexafluorophosphate Chemical Structure

Gamitrinib TPP hexafluorophosphate Chemical Structure

CAS No. : 1131626-47-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 2165 In-stock
Solution
10 mM * 1 mL in DMSO USD 2165 In-stock
Solid
1 mg USD 350 In-stock
5 mg USD 950 In-stock
10 mg USD 1520 In-stock
25 mg USD 3050 In-stock
50 mg USD 4850 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Gamitrinib TPP hexafluorophosphate:

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Gamitrinib TPP hexafluorophosphate is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP hexafluorophosphate is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.

IC50 & Target

HSP90

 

In Vitro

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.

In Vivo

Whether the combination of TRAIL plus Gamitrinib TPP (GamitrinibTPP, 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.
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)

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
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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 98.52%

References
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

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
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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Gamitrinib TPP hexafluorophosphate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Gamitrinib TPP hexafluorophosphate
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HY-102007A
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