| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
SDZ-LAP-977 targets tubulin, a key protein involved in the formation of microtubules, which are essential for cell division. By binding to the colchicine binding site on tubulin, SDZ-LAP-977 inhibits tubulin polymerization, thereby preventing the formation of mitotic spindles. This disruption of microtubule dynamics leads to cell cycle arrest and apoptosis in rapidly dividing cancer cells. The compound also exhibits activity as an EGF receptor tyrosine kinase inhibitor, although its primary mechanism of action is through tubulin binding.
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| ln Vitro |
In nude mice bearing the human tumor cell lines A431 (vulvar cancer cells), MIA PaCa-2 (pancreatic tumor cells), and MDA-MB-231 (breast cancer cells), the anticancer activities of SDZ 281-977 were investigated. The reason for selecting these cell lines is their sensitivity to SDZ 281-977. The proliferation of A431, MIA PaCa-2, and MDA-MB-231 cells can be inhibited with IC50 values of 0.21 μM, 0.29 μM, and 0.43 μM, respectively [1].
In vitro, SDZ-LAP-977 acts as an antiproliferative agent by binding to the colchicine binding site on tubulin and inhibiting tubulin polymerization. It inhibits the growth of human vulvar cancer cells and other cancer cell lines. The compound's ability to disrupt microtubule dynamics and induce cell cycle arrest has been confirmed in cell-based assays. These in vitro studies demonstrate the compound's anticancer activity. |
| ln Vivo |
During four weeks, intravenous injections of SDZ 281-977 (1–10 mg/kg) were administered to nude mice harboring A431 human vulvar carcinoma. Tumor growth was inhibited in a dose-dependent manner as a result of this treatment. After three weeks of treatment, oral dosing of SDZ 281-977 (30 mg/kg) reduced the growth of A431 tumors by 54%. The aforementioned regimen was highly received. Body weight did not significantly alter while receiving treatment [1].
In vivo, SDZ-LAP-977 has been investigated in nude mice bearing human tumor cell lines A431 (vulvar carcinoma), MIA PaCa-2 (pancreatic tumor), and MDA-MB-231 (breast carcinoma). The compound's anticancer profile has been evaluated in these xenograft models, demonstrating its ability to inhibit tumor growth. These in vivo studies support the compound's potential as an anticancer agent. |
| Enzyme Assay |
The in vitro enzyme/receptor binding (non-cellular) assays for SDZ-LAP-977 include tubulin polymerization assays. In these assays, purified tubulin is incubated with varying concentrations of SDZ-LAP-977, and the extent of tubulin polymerization is measured spectrophotometrically. The compound's ability to inhibit polymerization is assessed. Additionally, the compound's ability to bind to the colchicine binding site on tubulin can be evaluated using competitive binding assays with radiolabeled colchicine.
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| Cell Assay |
In vitro cellular assays for SDZ-LAP-977 are performed using cancer cell lines, including vulvar carcinoma cells (A431), pancreatic tumor cells (MIA PaCa-2), and breast carcinoma cells (MDA-MB-231). Cells are treated with varying concentrations of SDZ-LAP-977, and cell viability is measured using MTT assays. Cell cycle distribution is analyzed by flow cytometry to assess mitotic arrest. Apoptosis is evaluated using annexin V staining or caspase activity assays. These assays confirm the antiproliferative and pro-apoptotic activities of SDZ-LAP-977.
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| Animal Protocol |
In vivo animal experiments for SDZ-LAP-977 are conducted in nude mice bearing human tumor xenografts. Mice are implanted with A431, MIA PaCa-2, or MDA-MB-231 tumor cells and treated with SDZ-LAP-977 via intraperitoneal or intravenous administration. Tumor growth inhibition is monitored, and endpoints include tumor volume, tumor weight, and survival. Histopathological analysis of tumor tissues may also be performed to assess the compound's effects on cell proliferation and apoptosis.
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| ADME/Pharmacokinetics |
SDZ-LAP-977 has a molecular weight of 316.35 g/mol and a molecular formula of C18H20O5. Detailed pharmacokinetic properties such as bioavailability, half-life, and tissue distribution have not been extensively reported in the available literature. As a derivative of lavendustin A, SDZ-LAP-977 may have limited oral bioavailability and may require parenteral administration for systemic delivery. Further pharmacokinetic studies would be necessary to support its development as a therapeutic agent.
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| Toxicity/Toxicokinetics |
The toxicological profile of SDZ-LAP-977 has not been extensively characterized. As a tubulin-binding agent, the compound may have potential toxicity to normal rapidly dividing cells, similar to other microtubule-targeting drugs. Standard toxicology studies, including assessment of cytotoxicity in normal cell lines and acute toxicity in animal models, would be necessary to establish its safety profile. The compound's selectivity for cancer cells over normal cells would be an important consideration for its therapeutic potential.
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| References |
[1]. Cammisuli S, et al. SDZ 281-977: a modified partial structure of lavendustin A that exerts potent and selective antiproliferative activities in vitro and in vivo. Int J Cancer. 1996 Jan 26;65(3):351-9
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| Additional Infomation |
SDZ-LAP-977 is a synthetic derivative of the EGF receptor tyrosine kinase inhibitor lavendustin A. It exhibits anticancer and antiproliferative activity by binding to the colchicine binding site on tubulin and inhibiting tubulin polymerization. The compound inhibits the growth of human vulvar carcinoma, pancreatic tumor, and breast carcinoma cells in vitro and in xenograft mouse models. SDZ-LAP-977 is a research compound with potential applications in cancer therapy. It is not an approved drug and requires further development.
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| Molecular Formula |
C18H20O5
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| Molecular Weight |
316.35
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| Exact Mass |
316.131
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| CAS # |
150779-71-8
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| PubChem CID |
9818362
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| Appearance |
White to off-white solid powder
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| LogP |
2.981
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
23
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| Complexity |
372
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(OC)C1=CC(CCC2=CC(OC)=CC=C2OC)=CC=C1O
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| InChi Key |
GZOFTOHENYHNMS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H20O5/c1-21-14-7-9-17(22-2)13(11-14)6-4-12-5-8-16(19)15(10-12)18(20)23-3/h5,7-11,19H,4,6H2,1-3H3
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| Chemical Name |
methyl 5-[2-(2,5-dimethoxyphenyl)ethyl]-2-hydroxybenzoate
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| Synonyms |
SDZLAP977; SDZ LAP 977; SDZ-LAP-977
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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 Vitro) |
DMSO : ~100 mg/mL (~316.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.90 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (7.90 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 25.0 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: ≥ 2.5 mg/mL (7.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1611 mL | 15.8053 mL | 31.6106 mL | |
| 5 mM | 0.6322 mL | 3.1611 mL | 6.3221 mL | |
| 10 mM | 0.3161 mL | 1.5805 mL | 3.1611 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.
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