| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
The Hsp90 ATPase inhibitory module of 17-allylaminogeldanamycin (17-AAG) and the mitochondrial moiety of tri-aldehyde binding are combined in gamitrinib TPP (G-TPP), a little molecule. TPP effectively destroys mitochondria and has no effect on the induction of Hsp90 outside of the organelle. Within 16 hours of exposure, patient-derived and cultivated cytoblastoma cell lines were indiscriminately destroyed by gamatrinib TPP at doses of 15–20 μM. With loss of membrane potential within the organelle, cytochrome c release in the cytoplasm, activation of promoter caspase-9 and effectors caspase-3 and caspase-7, and annexin V. Reactivity, this cell death response is typical of mitochondria[1].
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| ln Vivo |
The potential for stellate anti-astroblastoma action of TRAIL plus Gamitrinib TPP (G-TPP) combo treatment was examined. The right brain striatum of immunocompromised mice has U87 astroblastoma cells that contain luciferase. These cells use bioluminescence to form tumors quickly. It is not ideal to treat these animals with a vehicle, TRAIL three-dimensional gradient descent, or systemic administration. Gamitrinib TPP concentrations had no effect on tumor development in vivo. Similarly, orthotopic astroblast tumor growth was unaffected by systemic monotherapy with gamitrinib TPP at a dose that reduces tumor growth in subcutaneous xenografts in mice (20 mg/kg, daily intraperitoneal injection). On the other hand, two rounds of intracranial tumor growth produced no results. Without significantly reducing the animal's body weight over the course of treatment, TRAIL in combination with systemic gamitrinib TPP inhibits the growth of established astroblastomas [1].
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| References |
| Molecular Formula |
C52H65F6N3O8P2
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|---|---|
| Molecular Weight |
1036.02575755119
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| Exact Mass |
1035.415
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| CAS # |
1131626-47-5
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| Related CAS # |
Gamitrinib TPP;1131626-46-4
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| PubChem CID |
25232581
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| Appearance |
Pale purple to purple solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
71
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| Complexity |
1750
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| Defined Atom Stereocenter Count |
6
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| SMILES |
[P+](C1C=CC=CC=1)(C1C=CC=CC=1)(C1C=CC=CC=1)CCCCCCNC1C(C=C2C(C=1C[C@@H](C)C[C@@H]([C@@H]([C@@H](C)C=C(C)[C@@H]([C@H](C=CC=C(C)C(N2)=O)OC)OC(N)=O)O)OC)=O)=O.[P-](F)(F)(F)(F)(F)F |c:44,49,51|
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| InChi Key |
NFIBTCZSRLMDOD-WLXHSWTPSA-O
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| InChi Code |
InChI=1S/C52H64N3O8P.F6P/c1-35-31-42-47(54-29-18-7-8-19-30-64(39-22-12-9-13-23-39,40-24-14-10-15-25-40)41-26-16-11-17-27-41)44(56)34-43(49(42)58)55-51(59)36(2)21-20-28-45(61-5)50(63-52(53)60)38(4)33-37(3)48(57)46(32-35)62-6;1-7(2,3,4,5)6/h9-17,20-28,33-35,37,45-46,48,50,57H,7-8,18-19,29-32H2,1-6H3,(H3-,53,54,55,56,58,59,60);/q;-1/p+1/b28-20-,36-21+,38-33+;/t35-,37+,45+,46+,48-,50+;/m1./s1
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| Chemical Name |
6-[[(4E,6Z,8S,9S,10E,12S,13R,14S,16R)-9-carbamoyloxy-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-19-yl]amino]hexyl-triphenylphosphanium;hexafluorophosphate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~48.26 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.41 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (2.41 mM) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
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