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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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5g |
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Other Sizes |
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Purity: ≥98%
Temozolomide (Methazolastone; CCRG81045; NSC 362856; SCH 52365; MB39831; and RP46161) is an orally bioavailable and brain penetrant DNA alkylating agent / damage inducer used as an anticancer drug. Methazolastone causes formation of DNA alkali-labile sites which are present in similar amounts and repaired at a similar rate in L-1210 and L-1210/BCNU cell lines. In L-1210 but not in L-1210/BCNU methazolastone induces an arrest of cells in SL-G2-M phases. Methazolastone sensitivity of both chemo-sensitive and resistant cells (D54-R and U87-R) is enhanced significantly under hyperoxia.
ln Vitro |
Temozolomide (TZM) is a methylating drug prescribed for metastatic melanoma and malignant glioma that is able to pass the blood-brain barrier. Temozolomide works well against tumor cells that have a functional mismatch repair system (MR) and low amounts of O6-alkylguanine DNA alkyltransferase (OGAT) [1]. Cell lines with low IC50 values (<50 μM), such as A172 (14.1±1.1 μM) and LN229 cells (14.5±1.1 μM), and those with high IC50 values (>100 μM), such as SF268 (147.2±2.1 μM) and SK-N-SH cells (234.6±2.3 μM), were found to have varying temozolomide (TZM) IC50 values in different cell lines ranging from 14.1 to 234.6 μM [3].
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ln Vivo |
Temozolomide (TZM) as a single drug did not significantly increase median survival time (MST) compared with controls. Notably, intracranial injection of NU1025 before administration of 100 or 200 mg/kg Temozolomide significantly increased longevity in the control or Temozolomide-only group. When temozolomide was divided, the lifespan extension (ILS) obtained with this regimen was higher than that observed when NU1025 was combined with a single injection of temozolomide (statistical comparison of survival curves: NU1025 intracranial injection + temozolomide 100 mg/kg×2 vs NU1025 + temozolomide 200 mg /kg; P=0.023)[1].
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Animal Protocol |
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References |
[1]. Tentori L, et al. Combined treatment with temozolomide and poly(ADP-ribose) polymerase inhibitor enhances survival of mice bearing hematologic malignancy at the central nervous system site. Blood. 2002 Mar 15;99(6):2241-4.
[2]. Mathieu V, et al. Combining Anti-Human VEGF with temozolomide increases the antitumor efficacy of temozolomide in a human glioblastoma orthotopic xenograft model. Neoplasia. 2008 Dec;10(12):1383-92. [3]. Perazzoli G, et al. Temozolomide Resistance in Glioblastoma Cell Lines: Implication of MGMT, MMR, P-Glycoprotein and CD133 Expression. PLoS One. 2015 Oct 8;10(10):e0140131 |
Molecular Formula |
C6H6N6O2
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Molecular Weight |
194.15
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CAS # |
85622-93-1
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Related CAS # |
Temozolomide-d3;208107-14-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1N(C([H])([H])[H])N=NC2=C(C(N([H])[H])=O)N=C([H])N21
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Synonyms |
CCRG81045, NSC362856; NSC 362856; CCRG 81045; NSC-362856; CCRG-81045; SCH-52365; SCH52365; SCH 52365; MB39831; MB-39831; MB 39831; RP46161; RP 46161; R-P46161; CCRG81045; TMZ. US trade names: Methazolastone; Temodar. Foreign brand name: Temodal
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (6.44 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 12.5 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: ≥ 1.25 mg/mL (6.44 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 12.5 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: ≥ 1.25 mg/mL (6.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO +30% PEG 300 +ddH2O: 2mg/mL Solubility in Formulation 5: 9.09 mg/mL (46.82 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 5.1507 mL | 25.7533 mL | 51.5066 mL | |
5 mM | 1.0301 mL | 5.1507 mL | 10.3013 mL | |
10 mM | 0.5151 mL | 2.5753 mL | 5.1507 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.