| Size | Price | Stock | Qty |
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| Targets |
DP-1 is a degradation product and fragment of ganetespib, which is a potent inhibitor of heat shock protein 90 (HSP90). As a degradation product, DP-1 is not expected to have significant pharmacological activity. The parent molecule ganetespib binds to the ATP-binding pocket of HSP90, disrupting its chaperone function and leading to the proteasomal degradation of client oncoproteins such as HER2, AKT, and mutant EGFR.
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| ln Vitro |
No independent in vitro pharmacological activity is reported for DP-1. Ganetespib, the parent HSP90 inhibitor, exhibits potent anti-proliferative activity across multiple cancer cell lines (breast, lung, leukemia) with IC50 values in the low nanomolar range. DP-1 is a degradation product and fragment of ganetespib. As a degradation product, DP-1 may retain some structural features but is not expected to have significant activity.
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| ln Vivo |
The degradation product of SDC-TRAP-0063, known as DP-1, is present in the heart, tumors, and plasma[1].
DP-1 is a degradation product of SDC-TRAP-0063 and a fragment of ganetespib. Ganetespib has demonstrated in vivo anti-tumor activity in xenograft models of breast, lung, and colon cancer. DP-1 may be present in plasma, tumor, and heart tissues following administration of SDC-TRAP-0063 or ganetespib, indicating some systemic exposure. However, its independent in vivo activity is not characterized. |
| Enzyme Assay |
For in vitro analytical method development, DP-1 is dissolved in an organic solvent such as DMSO or methanol to prepare a stock solution (e.g., 1 mg/mL). The degradation product standard is then diluted to working concentrations (e.g., 1-100 ug/mL) for high-performance liquid chromatography (HPLC) or LC-MS analysis. The standard is used to establish the retention time, mass spectral characteristics, and peak purity for stability-indicating assays of ganetespib.
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| Cell Assay |
For in vitro cellular experiments, DP-1 is not used as an independent treatment but as an analytical standard for quantifying this degradation product in cell culture samples from cells treated with ganetespib. After sample collection, the DP-1 standard is spiked into the samples at a fixed concentration. Following protein precipitation with methanol or acetonitrile and centrifugation, samples are analyzed by LC-MS/MS to determine if DP-1 is formed as a cellular degradation product of ganetespib under culture conditions.
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| Animal Protocol |
For in vivo animal studies, DP-1 is not administered to animals independently. It is used as an analytical standard for quantifying this degradation product in plasma, tumor, and heart samples from animals dosed with SDC-TRAP-0063 or ganetespib. After sample collection, the DP-1 standard is spiked into the samples at a known concentration. Following extraction and LC-MS/MS analysis, the concentration of DP-1 is determined to support biotransformation studies and assess the in vivo stability of the parent drug.
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| ADME/Pharmacokinetics |
As a degradation product, DP-1 has no independent pharmacokinetic parameters. The parent drug ganetespib has been studied in clinical trials, with a half-life of approximately 4-6 hours in humans, high plasma protein binding (∼97%), and a volume of distribution of ∼200 L. DP-1 has been detected in plasma, tumor, and heart tissues following administration, indicating that it has some systemic exposure and tissue distribution but likely different PK properties compared to the parent molecule.
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| Toxicity/Toxicokinetics |
DP-1 is a research-use degradation product standard with no specific toxicity data available. Ganetespib as an HSP90 inhibitor has been studied in clinical trials for cancer, with common toxicities including diarrhea, fatigue, hepatotoxicity, and thrombocytopenia. DP-1, as a degradation product, is not intended for therapeutic use and is handled at milligram or microgram levels in analytical laboratories. Standard laboratory safety precautions for handling organic compounds (gloves, safety glasses, fume hood) are recommended. Not for human consumption.
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| References |
[1]. Chimmanamada DU, et, al. Targeted therapeutics. US20140079636A1.
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| Additional Infomation |
DP-1 is not a drug but a research-use degradation product and analytical standard. It has no approved therapeutic status and is not intended for human use. This compound is used for analytical method development, stability studies of HSP90 inhibitors, and biotransformation research. DP-1 is a degradation product of SDC-TRAP-0063 and a fragment of ganetespib, a heat shock protein 90 (HSP90) inhibitor with anti-tumor activity. The compound is used in biochemical and in vitro studies of HSP90-related pathways and as a reference standard in pharmaceutical quality control.
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| Molecular Formula |
C26H31N5O3
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|---|---|
| Molecular Weight |
461.56
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| Exact Mass |
461.242
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| CAS # |
1472616-61-7
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| PubChem CID |
136377208
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| Appearance |
White to off-white solid powder
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| LogP |
3.7
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
755
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)C1=C(C=C(C(=C1)C2=NNC(=O)N2C3=CC4=C(C=C3)N(C=C4)CCC5CCNCC5)O)O
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| InChi Key |
CPMBELNSUCVCNT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H31N5O3/c1-16(2)20-14-21(24(33)15-23(20)32)25-28-29-26(34)31(25)19-3-4-22-18(13-19)8-12-30(22)11-7-17-5-9-27-10-6-17/h3-4,8,12-17,27,32-33H,5-7,9-11H2,1-2H3,(H,29,34)
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| Chemical Name |
3-(2,4-dihydroxy-5-propan-2-ylphenyl)-4-[1-(2-piperidin-4-ylethyl)indol-5-yl]-1H-1,2,4-triazol-5-one
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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: 25 mg/mL (54.16 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.42 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (5.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1666 mL | 10.8328 mL | 21.6657 mL | |
| 5 mM | 0.4333 mL | 2.1666 mL | 4.3331 mL | |
| 10 mM | 0.2167 mL | 1.0833 mL | 2.1666 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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