| Size | Price | Stock | Qty |
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| Other Sizes |
Purity: ≥98%
| Targets |
Satraplatin targets DNA, forming platinum-DNA adducts that crosslink DNA and induce apoptosis in cancer cells. As a platinum(IV) prodrug, it is reduced intracellularly to the active platinum(II) species, which then binds to DNA. It is more hydrophobic than cisplatin or oxaliplatin.
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| ln Vitro |
Satraplatin is unstable in an alkaline state but stable in an acidic state, thus it must be kept away from light in the solution.
Satraplatin exhibits strong antitumor properties. With an IC50 of 1.36 ± 0.11 μM, satraplatin inhibits UMC-11 cells when combined with dichloroacetate (DCA)[1]. Additionally, satraplatin causes G2/M arrest in KB-R cells and suppresses CDDP-resistant (KB-R) cells (IC50, 7.04 μM)[2]. Satraplatin (JM216) and its metabolite JM118 demonstrated cytotoxic activity against lung carcinoid cell lines. Against H727 cells, IC50 for satraplatin was below the achievable peak plasma concentration (1.4 μM). H835 cells grown as single cell suspensions were sensitive to satraplatin and its metabolites, while H835 multicellular spheroids showed increased resistance: 7.9-fold resistance to satraplatin and 8.7-fold resistance to JM118 compared to single cell suspensions. In the highly chemoresistant UMC-11 cell line, satraplatin exhibited an IC50 of 7.8±0.4 μM in the presence of 10 mM dichloroacetate (DCA), and DCA sensitized UMC-11 cells to satraplatin with a sensitization factor of 1.36±0.11 (i.e., IC50 in medium alone divided by IC50 with DCA). [1] Satraplatin is an alkylating agent with anti-tumor activity. It forms DNA adducts that inhibit DNA replication and transcription, leading to cell cycle arrest and apoptosis. The compound is active against a range of cancer cell lines, including those resistant to cisplatin. In vitro studies require protection from light due to instability in alkaline conditions. |
| ln Vivo |
Satraplatin has been investigated in clinical trials for the treatment of prostate cancer, lung cancer, and solid tumors. As an orally available platinum analog, it offers the advantage of convenient outpatient administration compared to intravenous platinum drugs. It has shown activity in hormone-refractory prostate cancer and other malignancies.
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| Enzyme Assay |
Cell-free DNA binding assays for Satraplatin involve incubating the compound with purified DNA (e.g., calf thymus DNA) and measuring platinum-DNA adduct formation. Adducts are quantified by atomic absorption spectroscopy or using radiolabeled platinum. Alternatively, the compound can be reduced chemically to the active platinum(II) species and its DNA binding properties characterized.
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| Cell Assay |
After being collected, cells are tallied and then added to 100 μL of medium in microtiter plates at a density of 1×104 cells per well. Test compounds (such as saprolactone) are diluted appropriately and added to each well, resulting in a total volume of 200 μL. The plates are then incubated for four days under tissue culture conditions. In order to prepare stock solutions for the assays, the compounds are diluted more than 100 times using either 70% ethanol or DMSO. Every test includes solvent controls. IC50 values are computed using dose response curves, which are produced by measuring cell proliferation in triplicate at twofold drug dilutions. The modified tetrazolium dye assay (MTT) and the reduced formazane dye measurement at 450 nm wavelength (with the medium control set to 100% proliferation) are two methods used to quantify cell growth[1].
Three permanent lung carcinoid cell lines (UMC-11, H727, H835) were used. Cells were seeded at 1×10^4 cells/well in microtiter plates and exposed to serial two-fold dilutions of satraplatin and its metabolites (JM149, JM118) for 4 days. Cell proliferation was quantified using a tetrazolium-based dye assay (MTT, EZ4U), measuring formazan absorbance at 450 nm. IC50 values were calculated from dose-response curves. For spheroid experiments, H835 cells were cultured as multicellular aggregates (150-250 μm diameter) and tested similarly. For combination studies, UMC-11 cells were treated with satraplatin in the continuous presence of 10 mM dichloroacetate (DCA), and IC50 values were compared to those without DCA to calculate sensitization factors. [1] Cancer cell lines (e.g., prostate, lung, ovarian cancer cells) are treated with Satraplatin at various concentrations for specified durations. Cell viability is assessed by MTT or CellTiter-Glo assays to determine IC50 values. DNA damage is assessed by γ-H2AX foci formation or comet assay. Cell cycle analysis and apoptosis assays (Annexin V staining, caspase activation) are performed to evaluate the mechanism of cell death. |
| Animal Protocol |
In vivo animal studies for Satraplatin were conducted in mouse xenograft models of various human cancers. The compound is administered orally at various doses. Tumor growth is measured over time, and tumor regression or growth inhibition is calculated. Pharmacodynamic markers (DNA adduct levels in tumor tissue) are assessed. Body weight and clinical signs are monitored for tolerability.
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| ADME/Pharmacokinetics |
Satraplatin is orally bioavailable. Following oral administration, it is absorbed and reduced to the active platinum(II) species. The compound is more lipophilic than cisplatin, which contributes to its oral bioavailability and altered tissue distribution. PK parameters including Tmax, half-life, clearance, and bioavailability have been characterized in preclinical species and humans.
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| Toxicity/Toxicokinetics |
Toxicity of Satraplatin is similar to other platinum drugs, including nephrotoxicity, myelosuppression (thrombocytopenia, neutropenia, anemia), nausea, vomiting, and peripheral neuropathy. The oral formulation may have a different toxicity profile compared to intravenous platinum drugs. Standard toxicological assessments have been conducted to support clinical development.
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| References | |
| Additional Infomation |
Satraplatin is an oral platinum(IV) complex (JM216) that is converted in vivo to active metabolites JM149 and JM118. It has shown promising clinical activity in lung cancer trials. The achievable peak plasma concentration (PPC) for satraplatin is 1.4 μM, and for its metabolite JM118 is 2.2 μM. In this study, satraplatin and JM118 were tested alongside other platinum drugs (picoplatin, oxaliplatin, carboplatin) against lung carcinoid cell lines. The authors conclude that satraplatin has potential for treatment of lung carcinoids. [1]
Satraplatin (molecular formula C10H22Cl2N2O4Pt, MW 500.3) is a platinum(IV) complex that was developed as an orally bioalternative to cisplatin. It was investigated in multiple clinical trials for prostate cancer, lung cancer, and other solid tumors. Despite promising activity, it did not receive regulatory approval. The compound is intended for research use only. |
| Molecular Formula |
C10H22CL2N2O4PT
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|---|---|
| Molecular Weight |
502.29256
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| Exact Mass |
499.06
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| Elemental Analysis |
C, 24.01; H, 4.43; Cl, 14.17; N, 5.60; O, 12.79; Pt, 38.99
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| CAS # |
129580-63-8
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| PubChem CID |
155491097
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| Appearance |
Off-white to yellow solid powder
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| Boiling Point |
134.5ºCat 760 mmHg
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| Flash Point |
32.2ºC
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| Vapour Pressure |
8.07mmHg at 25°C
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| LogP |
3.706
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Heavy Atom Count |
19
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| Complexity |
71.7
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Pt+4](N)([Cl-])([Cl-])([O-]C(=O)C)([O-]C(=O)C)NC1CCCCC1
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| InChi Key |
CKNPWBAXEKSCRG-UHFFFAOYSA-J
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| InChi Code |
InChI=1S/C6H13N.2C2H4O2.2ClH.H3N.Pt/c7-6-4-2-1-3-5-6;2*1-2(3)4;;;;/h6H,1-5,7H2;2*1H3,(H,3,4);2*1H;1H3;/q;;;;;;+4/p-4
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| Chemical Name |
(OC-6-43)-bis(acetato)amminedichloro(cyclohexylamine)platinum
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| Synonyms |
Satraplatin; BMS182751; BMS-182751; BMS 182751; JM216; JM 216; JM-216
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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) |
DMF: ~10 mg/mL (~20 mM)
H2O: < 0.1 mg/mL Ethanol: < 1 mg/mL |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9909 mL | 9.9544 mL | 19.9088 mL | |
| 5 mM | 0.3982 mL | 1.9909 mL | 3.9818 mL | |
| 10 mM | 0.1991 mL | 0.9954 mL | 1.9909 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03258320 | Recruiting | Drug: Cabazitaxel, Docetaxel, Mitoxantrone or Satraplatin |
Prostate Cancer Patients | Shanghai Jiao Tong University School of Medicine |
January 2015 | Phase 1 |
| NCT01289067 | Completed | Drug: Satraplatin | Prostate Cancer | William K. Oh | December 2010 | Phase 2 |
| NCT00370383 | Completed | Drug: Erlotinib Drug: Satraplatin |
Lung Cancer | Agennix | July 2006 | Phase 2 |
| NCT00499694 | Completed | Biological: bevacizumab Drug: satraplatin |
Prostate Cancer | Barbara Ann Karmanos Cancer Institute |
October 2007 | Not Applicable |
| NCT00473720 | Completed | Drug: Satraplatin Drug: Abraxane |
Advanced Cancers | Yale University | May 2007 | Phase 1 |
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