MTIC
Based on 1 Customer Validation
MTIC, the active metabolite of Temozolomide (TMZ), is a DNA alkylating agent. MTIC has antitumor activity .
For research use only. We do not sell to patients.
- Purity: 98.83%
- CAS No.: 3413-72-7
- Formula: C5H8N6O
- Molecular Weight:168.16
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Biological Activity
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| GM892A cell line | IC50 |
5 μM
Compound: 4
|
In vitro cytotoxicity against human lymphoblastoid cell (GM892 A)
In vitro cytotoxicity against human lymphoblastoid cell (GM892 A)
|
[PMID: 7739008] |
| Raji | IC50 |
101 μM
Compound: 4
|
In vitro cytotoxicity against Raji cell line
In vitro cytotoxicity against Raji cell line
|
[PMID: 7739008] |
| SNB-19 | GI50 |
466 μM
Compound: 3; MTIC
|
Growth inhibition of MGMT-transfected human SNB19 cells after 7 days by MTT assay
Growth inhibition of MGMT-transfected human SNB19 cells after 7 days by MTT assay
|
10.1039/C6MD00384B |
| SNB-19 | GI50 |
472 μM
Compound: 2; MTIC
|
Growth inhibition of MGMT-transfected human SNB19 cells expressing MGMT after 7 days by MTT assay
Growth inhibition of MGMT-transfected human SNB19 cells expressing MGMT after 7 days by MTT assay
|
[PMID: 30108945] |
| SNB-19 | GI50 |
48.5 μM
Compound: 2; MTIC
|
Growth inhibition of vehicle-transfected human SNB19 cells after 7 days by MTT assay
Growth inhibition of vehicle-transfected human SNB19 cells after 7 days by MTT assay
|
[PMID: 30108945] |
| SNB-19 | GI50 |
48.5 μM
Compound: 3; MTIC
|
Growth inhibition of empty vector transfected human SNB19 cells after 7 days by MTT assay
Growth inhibition of empty vector transfected human SNB19 cells after 7 days by MTT assay
|
10.1039/C6MD00384B |
| U-373MG ATCC | GI50 |
398 μM
Compound: 2; MTIC
|
Growth inhibition of MGMT-transfected human U373 cells expressing MGMT after 7 days by MTT assay
Growth inhibition of MGMT-transfected human U373 cells expressing MGMT after 7 days by MTT assay
|
[PMID: 30108945] |
| U-373MG ATCC | GI50 |
398 μM
Compound: 3; MTIC
|
Growth inhibition of MGMT-transfected human U373 cells after 7 days by MTT assay
Growth inhibition of MGMT-transfected human U373 cells after 7 days by MTT assay
|
10.1039/C6MD00384B |
| U-373MG ATCC | GI50 |
93.7 μM
Compound: 2; MTIC
|
Growth inhibition of vehicle-transfected human U373 cells after 7 days by MTT assay
Growth inhibition of vehicle-transfected human U373 cells after 7 days by MTT assay
|
[PMID: 30108945] |
| U-373MG ATCC | GI50 |
93.7 μM
Compound: 3; MTIC
|
Growth inhibition of empty vector transfected human U373 cells after 7 days by MTT assay
Growth inhibition of empty vector transfected human U373 cells after 7 days by MTT assay
|
10.1039/C6MD00384B |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3413-72-7
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Appearance Solid
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Molecular Weight 168.16
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Formula C5H8N6O
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Color Off-white to pink
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SMILES
O=C(C1=C(/N=N/NC)N=CN1)N
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 25 mg/mL (148.67 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (14.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (14.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Ramalho MJ, et al. Biophysical interaction of temozolomide and its active metabolite with biomembrane models: The relevance of drug-membrane interaction for Glioblastoma Multiforme therapy. Eur J Pharm Biopharm. 2019;136:156-163. [Content Brief]
[2]. Nagasawa HT, et al. The mechanism of alkylation of DNA by 5-(3-methyl-1-triazeno)imidazole-4-carboxamide (MIC), a metabolite of DIC (NSC-45388). Non-involvement of diazomethane. Chem Biol Interact. 1974 Jun;8(6):403-13. [Content Brief]
[3]. Tsang LL, et al. Comparison of the cytotoxicity in vitro of temozolomide and dacarbazine, prodrugs of 3-methyl-(triazen-1-yl)imidazole-4-carboxamide. Cancer Chemother Pharmacol. 1991;27(5):342-6. [Content Brief]
[4]. Beal DD, et al. Carcinogenicity of the antineoplastic agent, 5-(3,3-dimethyl-1-triazeno)-imidazole-4-carboxamide, and its metabolites in rats. J Natl Cancer Inst. 1975 Apr;54(4):951-7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.9467 mL | 29.7336 mL | 59.4672 mL | 148.6679 mL |
| 5 mM | 1.1893 mL | 5.9467 mL | 11.8934 mL | 29.7336 mL | |
| 10 mM | 0.5947 mL | 2.9734 mL | 5.9467 mL | 14.8668 mL | |
| 15 mM | 0.3964 mL | 1.9822 mL | 3.9645 mL | 9.9112 mL | |
| 20 mM | 0.2973 mL | 1.4867 mL | 2.9734 mL | 7.4334 mL | |
| 25 mM | 0.2379 mL | 1.1893 mL | 2.3787 mL | 5.9467 mL | |
| 30 mM | 0.1982 mL | 0.9911 mL | 1.9822 mL | 4.9556 mL | |
| 40 mM | 0.1487 mL | 0.7433 mL | 1.4867 mL | 3.7167 mL | |
| 50 mM | 0.1189 mL | 0.5947 mL | 1.1893 mL | 2.9734 mL | |
| 60 mM | 0.0991 mL | 0.4956 mL | 0.9911 mL | 2.4778 mL | |
| 80 mM | 0.0743 mL | 0.3717 mL | 0.7433 mL | 1.8583 mL | |
| 100 mM | 0.0595 mL | 0.2973 mL | 0.5947 mL | 1.4867 mL |