SDZ281-977
Based on 1 Customer Validation
SDZ 281-977 is a derivative of the EGF receptor tyrosine kinase inhibitor Lavendustin A.
For research use only. We do not sell to patients.
- Purity: 98.00%
- CAS No.: 150779-71-8
- Formula: C18H20O5
- Molecular Weight:316.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
213 nM
Compound: 13
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Inhibition of A431 cell proliferation
Inhibition of A431 cell proliferation
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[PMID: 7990108] |
| B16 | IC50 |
269 nM
Compound: 13
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Inhibition of B16F1 cell proliferation
Inhibition of B16F1 cell proliferation
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[PMID: 7990108] |
| HaCaT | IC50 |
0.04 μM
Compound: 13
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Inhibitory activity of HaCaT keratinocyte cell line
Inhibitory activity of HaCaT keratinocyte cell line
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[PMID: 7990108] |
| HaCaT | IC50 |
47 nM
Compound: 1, SDZ LAP 977
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Antiproliferative activity against human HaCaT cells after 3 days by sulforhodamine B assay
Antiproliferative activity against human HaCaT cells after 3 days by sulforhodamine B assay
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[PMID: 18678497] |
| HeLa | IC50 |
470 nM
Compound: 13
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Inhibition of HeLa cell proliferation
Inhibition of HeLa cell proliferation
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[PMID: 7990108] |
| K562 | IC50 |
217.5 nM
Compound: 13
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Inhibition of K562 cell proliferation
Inhibition of K562 cell proliferation
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[PMID: 7990108] |
| KB | IC50 |
191.5 nM
Compound: 13
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Inhibition of KB cell proliferation
Inhibition of KB cell proliferation
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[PMID: 7990108] |
| L1210 | IC50 |
415 nM
Compound: 13
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Inhibition of L1210 cell proliferation
Inhibition of L1210 cell proliferation
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[PMID: 7990108] |
| LoVo | IC50 |
185 nM
Compound: 13
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Inhibition of LOVO cell proliferation
Inhibition of LOVO cell proliferation
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[PMID: 7990108] |
| MCF7 | IC50 |
19 nM
Compound: 13
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Inhibition of MCF-7 cell proliferation
Inhibition of MCF-7 cell proliferation
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[PMID: 7990108] |
| MDA-MB-231 | IC50 |
427.5 nM
Compound: 13
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Inhibition of MDA-MB-231 cell proliferation
Inhibition of MDA-MB-231 cell proliferation
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[PMID: 7990108] |
| MDA-MB-468 | IC50 |
46.5 nM
Compound: 13
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Inhibition of MDA-MB-468 cell proliferation
Inhibition of MDA-MB-468 cell proliferation
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[PMID: 7990108] |
| P388 | IC50 |
337.5 nM
Compound: 13
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Inhibition of P388 cell proliferation
Inhibition of P388 cell proliferation
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[PMID: 7990108] |
| SCL-1 | IC50 |
383 nM
Compound: 13
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Inhibition of SCL-1 cell proliferation
Inhibition of SCL-1 cell proliferation
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[PMID: 7990108] |
| SK-BR-3 | IC50 |
31 nM
Compound: 13
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Inhibition of SK-BR-3 cell proliferation
Inhibition of SK-BR-3 cell proliferation
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[PMID: 7990108] |
| U-937 | IC50 |
320 nM
Compound: 13
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Inhibition of U937 cell proliferation
Inhibition of U937 cell proliferation
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[PMID: 7990108] |
The anticancer profile of SDZ 281-977 is investigated in nude mice bearing the human tumor cell lines A431 (vulvar carcinoma cells), MIA PaCa-2 (pancreatic tumor cells) and MDA-MB-231 (breast carcinoma cells). These cell lines are selected because of their sensitivity for SDZ 281-977. The IC50 values for inhibition of growth of A431, MIA PaCa-2 and MDA-MB-231 cells are 0.21 μM, 0.29 μM and 0.43 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 150779-71-8
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Appearance Solid
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Molecular Weight 316.35
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Formula C18H20O5
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Color White to off-white
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SMILES
O=C(OC)C1=CC(CCC2=CC(OC)=CC=C2OC)=CC=C1O
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Synonyms
SDZ-LAP 977
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (316.11 mM; Need ultrasonic; 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. 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. 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 (7.90 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 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 (7.90 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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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
Tumor cell lines are grown at 37°C under optimal medium and cell concentration conditions in the absence of antibiotics. At the time of exponential growth for tumor cell lines growing in suspension or at the time of 60-90% confluence for adherent cell lines, cells are harvested (adherent cell lines are trypsinized), suspended in fresh growth medium and seeded into 96-well cell culture plates at concentrations ranging between 1000 and 5000 cells/well. Cells are grown at optimal initial concentration for 3-4 days in a final volume of 0.2 ml/well in the presence of graded concentrations of test compounds. Extent of cellular proliferation is measured by a colorimetric assay using MTT for cells growing in suspension or by sulforhodamine B (SRB) for adherent cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Female nude mice (nu/nu IFFA C BALB A) weighing 20-23 g are used. For i.v. studies, SDZ 281-977 (10 mg) is dissolved in 1 mL Vepesid solvent (3250 mg PEG 300, 10 mg citric acid, 400 mg Tween 80 and 1205 mg ethanol). This solution is diluted with saline or Vepesid solvent/saline 1:10 so that all animals intravenously receive 0.2 mL of 1:10 Vepesid solvent containing 1, 3 and 10 mg SDZ 281-977/kg. Higher doses are not given due to limited solubility. SDZ 281-977 is injected into the tail vein 3 or 4 times a week. For oral testing, SDZ 281-977 is dissolved in Placebo G (18% ethanol, 43% Labrafil M2125CS and 39% corn oil) and 0.2 mL is given orally with a gavage. Control animals are treated with the vehicle only. For the comparative experiments, standard anticancer drugs are dissolved in saline containing 1% Tween 80 and water, respectively, and are injected i.p. once a day for 4 days in a row. Treatment started 2 days after animals have been randomized.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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. 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 | 3.1611 mL | 15.8053 mL | 31.6106 mL | 79.0264 mL |
| 5 mM | 0.6322 mL | 3.1611 mL | 6.3221 mL | 15.8053 mL | |
| 10 mM | 0.3161 mL | 1.5805 mL | 3.1611 mL | 7.9026 mL | |
| 15 mM | 0.2107 mL | 1.0537 mL | 2.1074 mL | 5.2684 mL | |
| 20 mM | 0.1581 mL | 0.7903 mL | 1.5805 mL | 3.9513 mL | |
| 25 mM | 0.1264 mL | 0.6322 mL | 1.2644 mL | 3.1611 mL | |
| 30 mM | 0.1054 mL | 0.5268 mL | 1.0537 mL | 2.6342 mL | |
| 40 mM | 0.0790 mL | 0.3951 mL | 0.7903 mL | 1.9757 mL | |
| 50 mM | 0.0632 mL | 0.3161 mL | 0.6322 mL | 1.5805 mL | |
| 60 mM | 0.0527 mL | 0.2634 mL | 0.5268 mL | 1.3171 mL | |
| 80 mM | 0.0395 mL | 0.1976 mL | 0.3951 mL | 0.9878 mL | |
| 100 mM | 0.0316 mL | 0.1581 mL | 0.3161 mL | 0.7903 mL |
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