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| 10mg |
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| 25mg |
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Purity: ≥98%
Darinaparsin (ZIO-101, SP-02) is a novel and potent mitochondrial-targeted small molecule and an organic arsenic that is being developed for the treatment of various hematologic and solid cancers. Intravenous darinaparsin showed evidence of clinical activity in malignant lymphoma, particularly peripheral T-cell lymphoma (PTCL), in a Phase II study conducted in the U.S. In order to treat PTCL, darinaparsin received Orphan Drug Designation in the U.S. and Europe. Solasia plans to apply for a similar designation in Japan. Inorganic arsenicals (iAs) in vivo produce darinaparsin, a highly toxic metabolic intermediate. When glutathione (GSH) levels are low, darinaparsin appears to produce volatile cytotoxic arsenic compounds, though the precise mechanism of action is unknown. In addition, this substance or its byproducts may initiate cell death by interrupting the G2/M phase of the cell cycle and may exhibit antiangiogenic effects. The arsenic compounds generated from darinaparsin disrupt mitochondrial bioenergetics, producing reactive oxygen species (ROS) and inducing ROS-mediated tumor cell apoptosis.
| ln Vitro |
Darinaparsin is cytotoxic to prostate cancer cell lines and live prostate cancer cells at low micromolar concentrations, and it has the important property of inhibiting the so-called tumor-initiating cells (TIC) subpopulations[1].
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| ln Vivo |
Darinaparsin reduces the ability of prostate cancer cells to initiate tumors and slows the growth of the castrate-resistant Du145 prostate tumor grown as a xenograft in mice[1].
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| References |
| Molecular Formula |
C12H22ASN3O6S
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|---|---|
| Molecular Weight |
411.30618
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| Exact Mass |
411.04453
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| Elemental Analysis |
C, 35.04; H, 5.39; As, 18.22; N, 10.22; O, 23.34; S, 7.80
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| CAS # |
69819-86-9
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| Related CAS # |
69819-86-9
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| Appearance |
White to off-white solid powder
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| SMILES |
C[As](C)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N
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| InChi Key |
JGDXFQORBMPJGR-YUMQZZPRSA-N
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| InChi Code |
InChI=1S/C12H22AsN3O6S/c1-13(2)23-6-8(11(20)15-5-10(18)19)16-9(17)4-3-7(14)12(21)22/h7-8H,3-6,14H2,1-2H3,(H,15,20)(H,16,17)(H,18,19)(H,21,22)/t7-,8-/m0/s1
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| Chemical Name |
(2S)-2-amino-5-[[(2R)-1-(carboxymethylamino)-3-dimethylarsanylsulfanyl-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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| Synonyms |
Darinaparsin; Zinapar; SP-02; SP 02; SP02; ZIO 101; ZIO101; ZIO-101
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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) |
H2O: ~62.5 mg/mL (~152.0)
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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 | 2.4313 mL | 12.1563 mL | 24.3126 mL | |
| 5 mM | 0.4863 mL | 2.4313 mL | 4.8625 mL | |
| 10 mM | 0.2431 mL | 1.2156 mL | 2.4313 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 |
| NCT01139346 | Completed | Drug: darinaparsin | Advanced Solid Tumors | Alaunos Therapeutics | June 2010 | Phase 1 |
| NCT00591396 | Completed | Drug: ZIO-101 (Darinaparsin) |
Solid Tumors | Alaunos Therapeutics | July 2005 | Phase 1 |
| NCT00303199 | Completed | Drug: ZIO-101 (Darinaparsin) |
Multiple Myeloma | Alaunos Therapeutics | July 2005 | Phase 1 Phase 2 |
| NCT00509782 | Completed | Drug: ZIO-101 | MSolid Tumors | M.D. Anderson Cancer Center | May 2005 | Phase 1 |
| NCT00421213 | Completed | Drug: Darinaparsin | Hematologic Neoplasms Bone Marrow Neoplasms |
Alaunos Therapeutics | December 2006 | Phase 1 |
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