ZM 336372
Based on 2 publication(s) in Google Scholar
ZM 336372 is a potent inhibitor of the protein kinase c-Raf. The IC50 value is 0.07 μM in the standard assay, which contains 0.1 mM ATP.
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- Purity: 98.03%
- CAS No.: 208260-29-1
- 화학식: C23H23N3O3
- 분자량:389.45
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ZM 336372
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Biological Activity
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C-Raf 0.07 μM (IC50, 0.1 mM ATP) |
ZM 336372 is a potent inhibitor of human c-Raf. The IC50 value is 0.07 μM in the standard assay, which contains 0.1 mM ATP. The IC50, decreases to 0.01μM at 0.025 mM ATP and increases to 0.9 μM at 2.5 mM ATP indicating that ZM 336372 is a competitive inhibitor with respect to ATP. ZM 336372 inhibits c-Raf tenfold more potently than B-Raf[1]. Cell proliferation analysis of ZM336372. 3,4-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide growth assay of H727 and BON treated as control, DMSO, and 100 μM ZM336372 to days 16 and 10, respectively. Both H727 and BON cell proliferation is inhibited in the presence of drug compared with controls. H727 cells treated with ZM336372 are growth suppressed, whereas control treatments have significantly more growth by day 6, continuing up to 16 days. A similar response is also seen in BON cells as growth suppression occurred as early as day 4 and was maintained out to day 10[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 208260-29-1
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Appearance Solid
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분자량 389.45
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화학식 C23H23N3O3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C)C(NC(C2=CC=C(O)C=C2)=O)=C1)C3=CC=CC(N(C)C)=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Death Discov
Dual role of PID1 in regulating apoptosis induced by distinct anticancer-agents through AKT/Raf-1-dependent pathway in hepatocellular carcinoma. [Abstract]2023 Apr 28;9(1):139. PMID: 37117198 -
Oncogene
RAF1 facilitates KIT signaling and serves as a potential treatment target for gastrointestinal stromal tumor. [Abstract]2024 May 17. PMID: 38760447
용액&용해도
DMSO : 50 mg/mL (128.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (6.42 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 (6.42 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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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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.
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.
Protocol
Proliferation of H727 and BON cells after treatment with ZM336372 is measured using a 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. Cells are trypsinized and plated in triplicate to 24-well plates and allowed to adhere overnight. Then, cells are treated with either 100 μM ZM336372 or DMSO (2%) and incubated. Media are changed every 2 days with new treatment. At each time point, cell growth rates are analyzed after the addition of 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reagent to the cultured cells. Absorbance is determined using spectrophotometer at a wavelength of 540 nm[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Hall-Jackson CA, et al. Paradoxical activation of Raf by a novel Raf inhibitor. Chem Biol. 1999 Aug;6(8):559-68. [Content Brief]
[2]. Van Gompel JJ, et al. ZM336372, a Raf-1 activator, suppresses growth and neuroendocrine hormone levels in carcinoid tumor cells. Mol Cancer Ther. 2005 Jun;4(6):910-7. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5677 mL | 12.8386 mL | 25.6772 mL | 64.1931 mL |
| 5 mM | 0.5135 mL | 2.5677 mL | 5.1354 mL | 12.8386 mL | |
| 10 mM | 0.2568 mL | 1.2839 mL | 2.5677 mL | 6.4193 mL | |
| 15 mM | 0.1712 mL | 0.8559 mL | 1.7118 mL | 4.2795 mL | |
| 20 mM | 0.1284 mL | 0.6419 mL | 1.2839 mL | 3.2097 mL | |
| 25 mM | 0.1027 mL | 0.5135 mL | 1.0271 mL | 2.5677 mL | |
| 30 mM | 0.0856 mL | 0.4280 mL | 0.8559 mL | 2.1398 mL | |
| 40 mM | 0.0642 mL | 0.3210 mL | 0.6419 mL | 1.6048 mL | |
| 50 mM | 0.0514 mL | 0.2568 mL | 0.5135 mL | 1.2839 mL | |
| 60 mM | 0.0428 mL | 0.2140 mL | 0.4280 mL | 1.0699 mL | |
| 80 mM | 0.0321 mL | 0.1605 mL | 0.3210 mL | 0.8024 mL | |
| 100 mM | 0.0257 mL | 0.1284 mL | 0.2568 mL | 0.6419 mL |
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