| 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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| Other Sizes |
Purity: ≥98%
| Targets |
INO-1001 targets poly (ADP-ribose) polymerase (PARP), a nuclear enzyme involved in DNA repair. PARP plays a critical role in the base excision repair pathway, which repairs single-strand DNA breaks. Inhibition of PARP leads to the accumulation of DNA strand breaks, which, if unrepaired, result in cell death, particularly in cells with defective homologous recombination repair, such as those with BRCA mutations.
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|---|---|
| ln Vitro |
In Chinese hamster chromosomal AA8 (CHO) cells, the IC50 of INO-1001 is 0.05 μM [1].
In vitro, INO-1001 inhibits PARP activity, leading to the accumulation of DNA damage. It enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death. In Chinese hamster ovary AA8 (CHO) cells, INO-1001 has an IC50 of 0.05 μM. This potent inhibition of PARP makes it an effective radiosensitizer. |
| ln Vivo |
In vivo, INO-1001 has antitumor effects and acts as a potent enhancer of radiation sensitivity. It sensitizes tumors to chemotherapy and radiation therapy by inhibiting DNA repair. Its chemosensitization and radiosensitization properties make it a valuable tool for studying combination therapies in cancer treatment.
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| Enzyme Assay |
PARP enzyme activity is measured using a biochemical assay with purified PARP enzyme and radiolabeled NAD+ as a substrate. INO-1001 is incubated with the enzyme, and the incorporation of radiolabeled ADP-ribose into acceptor proteins is measured to calculate the IC50.
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| Cell Assay |
Radiosensitization is assessed in cultured cancer cell lines. Cells are treated with INO-1001 and exposed to ionizing radiation. Cell survival is measured using clonogenic assays, and DNA damage is assessed by comet assay or γ-H2AX foci formation.
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| Animal Protocol |
In vivo efficacy is evaluated in mouse xenograft models. INO-1001 is administered alone or in combination with radiation or chemotherapy. Tumor growth delay is measured, and markers of DNA damage and apoptosis are assessed.
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| ADME/Pharmacokinetics |
INO-1001 is expected to have good oral bioavailability and to distribute to tumor tissues. Its pharmacokinetic properties are consistent with other PARP inhibitors, supporting its use in combination with DNA-damaging therapies. It is soluble in DMSO at 31.25 mg/mL.
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| Toxicity/Toxicokinetics |
Potential toxicities of PARP inhibitors include myelosuppression, gastrointestinal effects (nausea, vomiting), and fatigue. Combination with radiation may exacerbate normal tissue toxicity. These effects are typically manageable with dose adjustments and supportive care.
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| References |
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| Additional Infomation |
See also: Ino-1001 (Note moved to).
INO-1001 is a research compound that has been investigated in preclinical and early clinical studies as a chemosensitizer and radiosensitizer for cancer therapy. Its potent and selective inhibition of PARP makes it a valuable tool for studying the role of PARP in DNA repair and for developing new cancer treatments that exploit synthetic lethality. |
| Molecular Formula |
C23H25N3O4S
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|---|---|
| Molecular Weight |
439.53
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| Exact Mass |
439.157
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| CAS # |
501364-82-5
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| Related CAS # |
501364-82-5
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| PubChem CID |
9889396
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.921
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
815
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CS(=O)(=O)O.C1COCCN1CCCNS(=O)(=O)C2=CC3=C(C=C2)C4=C(C3)C5=CC=CC=C5C(=O)N4
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| InChi Key |
LTZVLHHIAUKGBP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25N3O4S/c27-23-20-5-2-1-4-19(20)21-15-16-14-17(6-7-18(16)22(21)25-23)31(28,29)24-8-3-9-26-10-12-30-13-11-26/h1-2,4-7,14,24H,3,8-13,15H2,(H,25,27)
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| Chemical Name |
N-(3-morpholinopropyl)-5-oxo-6,11-dihydro-5H-indeno[1,2-c]isoquinoline-9-sulfonamide
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| Synonyms |
IN01001 INO-1001 INO 1001
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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 : ~31.25 mg/mL (~71.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 20.8 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: ≥ 2.08 mg/mL (4.73 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 | 2.2752 mL | 11.3758 mL | 22.7516 mL | |
| 5 mM | 0.4550 mL | 2.2752 mL | 4.5503 mL | |
| 10 mM | 0.2275 mL | 1.1376 mL | 2.2752 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.
Link: https://clinicaltrials.gov/ct2/show/NCT00271167
Conditions:Heart Diseases|Postoperative ComplicationsLink: https://clinicaltrials.gov/ct2/show/NCT00272415
Conditions:MelanomaLink: https://clinicaltrials.gov/ct2/show/NCT00271765
Conditions:Acute Myocardial InfarctionProducts are for research use only; We do not sell to patients
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