| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| Targets |
TDRL-551 targets replication protein A (RPA), an essential single-stranded DNA (ssDNA) binding protein complex in eukaryotes. RPA plays a crucial role in multiple key biological processes such as DNA replication, nucleotide excision repair (NER), homologous recombination (HR), telomere maintenance, and viral defense. By inhibiting RPA-DNA interaction, TDRL-551 disrupts these essential DNA metabolic processes.
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| ln Vitro |
In vitro, TDRL-551 is a potent RPA inhibitor with an IC50 of 18 µM. It inhibits RPA-DNA interaction and increases the anticancer efficacy of platinum-based chemotherapy. The compound is used in research to study the role of RPA in DNA repair and replication, and to investigate strategies for sensitizing cancer cells to DNA-damaging agents.
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| ln Vivo |
In vivo, TDRL-551 improves the efficacy of platinum-based chemotherapy for lung and ovarian cancer. By inhibiting RPA, the compound sensitizes tumors to platinum-based chemotherapeutics, enhancing their anticancer efficacy. It has been studied in preclinical models of non-small cell lung cancer (NSCLC) and ovarian cancer, demonstrating potential as a chemosensitizing agent.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for TDRL-551 measure its inhibition of RPA-DNA interaction. The assay typically involves incubating RPA protein with labeled DNA substrates in the presence of varying concentrations of the compound. The extent of RPA-DNA binding is quantified by electrophoretic mobility shift assays (EMSA) or fluorescence polarization. The IC50 of 18 µM is determined from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for TDRL-551 use cancer cell lines such as non-small cell lung cancer (NSCLC) cells. Cells are treated with serial dilutions of the compound, and the effects on cell viability, proliferation, and sensitivity to platinum-based chemotherapy are assessed using MTT or colony formation assays. The compound's ability to inhibit RPA function is confirmed by measuring DNA repair capacity or replication fork progression in treated cells.
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| ADME/Pharmacokinetics |
TDRL-551 has a molecular weight of 591.83 and a molecular formula of C25H23ClIN3O4. It is soluble in DMSO at approximately 62.5 mg/mL (~105.60 mM). For in vivo administration, the compound can be formulated in 10% DMSO + 90% corn oil at ≥2.08 mg/mL (3.51 mM). The compound is stored as a powder at -20°C for up to 3 years or in solution at -80°C for up to 6 months.
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| Toxicity/Toxicokinetics |
Toxicity data for TDRL-551 are available from preclinical safety studies. As an RPA inhibitor, the compound's toxicity profile is assessed in standard toxicology studies. The compound is for research use only and not for human use. Appropriate safety precautions should be taken during handling. The no-observed-adverse-effect level (NOAEL) and maximum tolerated dose (MTD) are determined from dose-escalation studies.
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| References | |
| Additional Infomation |
TDRL-551 is a research compound used to study the role of replication protein A (RPA) in DNA repair and replication. It is a novel small-molecule antiviral agent under investigation for its potential to treat viral infections, designed to inhibit the replication of specific viruses by targeting critical viral proteins or host factors essential for the viral life cycle. The compound is not approved for clinical use.
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| Molecular Formula |
C25H23CLIN3O4
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|---|---|
| Molecular Weight |
591.83
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| Exact Mass |
591.042
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| CAS # |
1644626-43-6
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| PubChem CID |
121336921
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
34
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| Complexity |
760
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(N1N=C(C2C=CC(I)=CC=2)CC1C1C(=NC2C=C(OCC)C=CC=2C=1)Cl)(=O)CCCC(=O)O
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| InChi Key |
QHNTZIUSUGGSNE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H23ClIN3O4/c1-2-34-18-11-8-16-12-19(25(26)28-20(16)13-18)22-14-21(15-6-9-17(27)10-7-15)29-30(22)23(31)4-3-5-24(32)33/h6-13,22H,2-5,14H2,1H3,(H,32,33)
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| Chemical Name |
5-(5-(2-chloro-7-ethoxyquinolin-3-yl)-3-(4-iodophenyl)-4,5-dihydro-1H-pyrazol-1-yl)-5-oxopentanoic acid
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| Synonyms |
TDRL 551 TDRL-551 TDRL551.
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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 : ~62.5 mg/mL (~105.60 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6897 mL | 8.4484 mL | 16.8967 mL | |
| 5 mM | 0.3379 mL | 1.6897 mL | 3.3793 mL | |
| 10 mM | 0.1690 mL | 0.8448 mL | 1.6897 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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