Size | Price | Stock | Qty |
---|---|---|---|
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
Other Sizes |
|
Venadaparib (IDX-1197; IDX1197) is a novel, selective and orally bioactive PARP inhibitor (IC50s = 1 ~2 nM) with anticancer activity. IDX-1197 converts SSBs into DSBs, or double-strand breaks, by blocking PARP, preventing cancer cells from repairing SSBs. IDX-1197 causes synthetic lethality, which is characterized by cell death brought on by simultaneous disruption of two genes without causing harm to healthy cells. Patients with homologous recombination deficiency (HRD) are the main target population for IDX-1197. The enzymes PARP1 and PARP2 are more successfully trapped on damaged DNA by IDX-1197, which is noteworthy for having a particularly strong trapping effect.
Targets |
PARP1 ( IC50 = 1.4 nM ); PARP2 ( IC50 = 1 nM )
|
---|---|
ln Vitro |
IDX-1197 strongly and specifically inhibits PARP1-mediated PAR expression in DNA damage-induced Hela cells, and does so without being sensitive to PARP5A (Tankyrase-1). [1]
|
ln Vivo |
IDX-1197 administered orally as opposed to the Olaparib treatment group, results in dose-dependently strong inhibition of tumor growth in the germline BRCA1-mutated ovarian cancer PDX model. This is demonstrated in tumor tissues.[1]
|
Animal Protocol |
germline BRCA1-mutated ovarian cancer PDX model
o.g. |
References |
Molecular Formula |
C23H23FN4O2
|
---|---|
Molecular Weight |
406.4527
|
Exact Mass |
406.18
|
Elemental Analysis |
C, 67.97; H, 5.70; F, 4.67; N, 13.78; O, 7.87
|
CAS # |
1681017-83-3
|
Related CAS # |
1681017-83-3; 1681020-60-9 (HCl)
|
Appearance |
Solid powder
|
SMILES |
C1CC1NCC2CN(C2)C(=O)C3=C(C=CC(=C3)CC4=NNC(=O)C5=CC=CC=C54)F
|
InChi Key |
YNBQAYKYNYRCCA-UHFFFAOYSA-N
|
InChi Code |
InChI=1S/C23H23FN4O2/c24-20-8-5-14(10-21-17-3-1-2-4-18(17)22(29)27-26-21)9-19(20)23(30)28-12-15(13-28)11-25-16-6-7-16/h1-5,8-9,15-16,25H,6-7,10-13H2,(H,27,29)
|
Chemical Name |
4-[[3-[3-[(cyclopropylamino)methyl]azetidine-1-carbonyl]-4-fluorophenyl]methyl]-2H-phthalazin-1-one
|
Synonyms |
Venadaparib; IDX1197; IDX 1197; IDX-1197
|
HS Tariff Code |
2934.99.9001
|
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)
|
Solubility (In Vitro) |
DMSO: ~81 mg/mL (~199.3 mM)
Ethanol: ~5 mg/mL |
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.75 mg/mL (14.15 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 57.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 5 mg/mL (12.30 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 50.0 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. View More
Solubility in Formulation 3: 5 mg/mL (12.30 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4603 mL | 12.3016 mL | 24.6033 mL | |
5 mM | 0.4921 mL | 2.4603 mL | 4.9207 mL | |
10 mM | 0.2460 mL | 1.2302 mL | 2.4603 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04174716 | Active Recruiting |
Drug: IDX-1197 | Solid Tumors | Idience Co., Ltd. | November 6, 2019 | Phase 1 Phase 2 |
NCT04725994 | Recruiting | Drug: IDX-1197+XELOX Drug: IDX-1197+Irinotecan |
Gastric Cancer | Idience Co., Ltd. | June 28, 2021 | Phase 1 |
NCT05202912 | Completed | Drug: IDX-1197(After a meal) Drug: IDX-1197(fasting) |
Healthy Male | Idience Co., Ltd. | January 16, 2022 | Phase 1 |
NCT03317743 | Completed | Drug: NOV140101 (IDX-1197) | Advanced Solid Tumors | Idience Co., Ltd. | August 29, 2017 | Phase 1 |