LQZ-7I
Based on 1 Customer Validation
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
For research use only. We do not sell to patients.
- Purity : 99.78%
- CAS No.: 195822-23-2
- Formula: C20H14F2N4
- Molecular Weight:348.35
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
Description
IC50 & Target
Survivin[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP C4-2 | IC50 |
2 μM
Compound: LQZ-7I; 7I
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Cytotoxicity against human C4-2 cells transfected with pcDNA3.1 assessed as reduction in cell viability measured after 72 hrs by methylene blue staining based assay
Cytotoxicity against human C4-2 cells transfected with pcDNA3.1 assessed as reduction in cell viability measured after 72 hrs by methylene blue staining based assay
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[PMID: 32421328] |
| LNCaP C4-2 | IC50 |
3.1 μM
Compound: LQZ-7I; 7I
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Cytotoxicity against human C4-2 cells assessed as reduction in cell viability measured after 72 hrs by methylene blue staining based assay
Cytotoxicity against human C4-2 cells assessed as reduction in cell viability measured after 72 hrs by methylene blue staining based assay
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[PMID: 32421328] |
| LNCaP C4-2 | IC50 |
3.1 μM
Compound: 9; LQZ-7I
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Cytotoxicity against human LNCaP C4-2 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
Cytotoxicity against human LNCaP C4-2 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
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[PMID: 38092421] |
| LNCaP C4-2 | IC50 |
7 μM
Compound: LQZ-7I; 7I
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Cytotoxicity against human C4-2 cells transfected with HA-tagged survivin assessed as reduction in cell viability measured after 72 hrs by methylene blue staining based assay
Cytotoxicity against human C4-2 cells transfected with HA-tagged survivin assessed as reduction in cell viability measured after 72 hrs by methylene blue staining based assay
|
[PMID: 32421328] |
| PC-3 | IC50 |
4.8 μM
Compound: LQZ-7I; 7I
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Cytotoxicity against human PC3 cells assessed as reduction in cell viability measured after 72 hrs by methylene blue staining based assay
Cytotoxicity against human PC3 cells assessed as reduction in cell viability measured after 72 hrs by methylene blue staining based assay
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[PMID: 32421328] |
| PC-3 | IC50 |
4.8 μM
Compound: 9; LQZ-7I
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Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
|
[PMID: 38092421] |
In Vitro
LQZ-7I has improved cytotoxicity with IC50s of 3.1 μM against C4-2 cells and 4.8 μM against PC-3 cells compared with the parent compound LQZ-7[1].
?
LQZ-7I (10 μM; 0-6 hours) treatment reduces the expression of survivin. However, LQZ-7I does not reduce the expression of XIAP, CIAP1, and CIAP2. LQZ-7I may be selective to its intended target survivin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:PC-3 or C4-2 cells
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Concentration:10 µM
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Incubation Time:0-6 hours
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Result:Reduced the expression of survivin.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week old male NSG mice[1]
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Dosage:100 mg/kg; 200 µL vehicle (90% corn oil/10% DMSO)
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Administration:Oral gavage every other day for a total of ten treatments
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Result:Significantly suppressed tumor growth without any notable adverse effect on the mice as indicated by lacking changes in body weight and in wet weight of major organs at the end of the study.
Chemical Information
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CAS No. 195822-23-2
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Appearance Solid
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Molecular Weight 348.35
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Formula C20H14F2N4
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Color Light yellow to green yellow
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SMILES
FC1=CC=C(NC2=NC3=CC=CC=C3N=C2NC4=CC=C(F)C=C4)C=C1
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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 2 years -20°C 1 year
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (358.83 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, 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)
In Vivo:
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.
In Vivo Dissolution Calculator
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.
Protocols
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Purity & Documentation
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Data Sheet (276 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
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 | 2.8707 mL | 14.3534 mL | 28.7068 mL | 71.7669 mL |
| 5 mM | 0.5741 mL | 2.8707 mL | 5.7414 mL | 14.3534 mL | |
| 10 mM | 0.2871 mL | 1.4353 mL | 2.8707 mL | 7.1767 mL | |
| 15 mM | 0.1914 mL | 0.9569 mL | 1.9138 mL | 4.7845 mL | |
| 20 mM | 0.1435 mL | 0.7177 mL | 1.4353 mL | 3.5883 mL | |
| 25 mM | 0.1148 mL | 0.5741 mL | 1.1483 mL | 2.8707 mL | |
| 30 mM | 0.0957 mL | 0.4784 mL | 0.9569 mL | 2.3922 mL | |
| 40 mM | 0.0718 mL | 0.3588 mL | 0.7177 mL | 1.7942 mL | |
| 50 mM | 0.0574 mL | 0.2871 mL | 0.5741 mL | 1.4353 mL | |
| 60 mM | 0.0478 mL | 0.2392 mL | 0.4784 mL | 1.1961 mL | |
| 80 mM | 0.0359 mL | 0.1794 mL | 0.3588 mL | 0.8971 mL | |
| 100 mM | 0.0287 mL | 0.1435 mL | 0.2871 mL | 0.7177 mL |