Size | Price | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
DNA Alkylator
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ln Vitro |
In order to prevent DNA strand separation during replication, phosphoramide mustard forms cross-linked DNA adducts, which are toxic[1]. In rat spontaneously immortalized granulosa cells (SIGCs), phosphoramide mustard (3-6 μM; 48 hours) decreases cell viability[1]. Ovarian DNA damage and DNA adduct formation are induced by mustard (3-6 μM; 24-48 hours)[1]. DNA damage responses (DDR) gene mRNA expression levels and DDR proteins are increased by phosphoramide mustard (3-6 μM; 24-48 hours)[1].
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ln Vivo |
In rats, phosphorus mustard (2.1-20.7 mg/kg; ip; daily; for 5 days) suppresses the formation of subcutaneous tumors[2]. After intravenous treatment, phosphoramide mustard has terminal elimination half-lives (rat 15.1 min; rat 59.4 mg/kg)[2].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: SIGCs Tested Concentrations: 0.5 μM, 1 μM, 3 μM, 6 μM Incubation Duration: 48 hrs (hours) Experimental Results: decreased cell viability at concentrations of 3 μM and higher. RT-PCR[1] Cell Types: SIGCs Tested Concentrations: 3 μM, 6 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: Increased DDR gene mRNA expression levels. Western Blot Analysis[1] Cell Types: SIGCs Tested Concentrations: 3 μM, 6 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours) Experimental Results: Generally increased DDR proteins. |
Animal Protocol |
Animal/Disease Models: Rat, subcutaneously (sc) implanted Walker 256 carcinosarcoma tumor[2]
Doses: 2.1 mg/kg, 4.8 mg/kg, 10.4 mg /kg, 20.7 mg/kg Route of Administration: intraperitoneal (ip)injection, one time/day, for 5 days Experimental Results: Required to produce 50% inhibition of subcutaneous (sc)tumor growth with dose of 12 mg/kg. Animal/Disease Models: Rats[2] Doses: 59.4 mg /kg (pharmacokinetic/PK Analysis) Route of Administration: intravenous (iv)injection Experimental Results: T1/2 (15.1 min). |
References |
[1]. Shanthi Ganesan, et al. Phosphoramide mustard exposure induces DNA adduct formation and the DNA damage repair response in rat ovarian granulosa cells. Toxicol Appl Pharmacol. 2015 Feb 1; 282(3): 252–258.
[2]. S Genka, et al. Brain and plasma pharmacokinetics and anticancer activities of cyclophosphamide and phosphoramide mustard in the rat. Cancer Chemother Pharmacol. 1990;27(1):1-7. |
Molecular Formula |
C4H11CL2N2O2P
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Molecular Weight |
221.02
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Exact Mass |
219.99
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CAS # |
10159-53-2
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Related CAS # |
Phosphoramide mustard cyclohexanamine;1566-15-0
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C(CCl)N(CCCl)P(=O)(N)O
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InChi Key |
RJXQSIKBGKVNRT-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C4H11Cl2N2O2P/c5-1-3-8(4-2-6)11(7,9)10/h1-4H2,(H3,7,9,10)
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Chemical Name |
amino-[bis(2-chloroethyl)amino]phosphinic acid
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Synonyms |
Phosphoramide mustard
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.5245 mL | 22.6224 mL | 45.2448 mL | |
5 mM | 0.9049 mL | 4.5245 mL | 9.0490 mL | |
10 mM | 0.4524 mL | 2.2622 mL | 4.5245 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.