A-620223
Based on 1 publication(s) in Google Scholar
A-620223 is a PARP-1 inhibitor with a Ki of 8 nM against PARP-1 and EC50 of 3 nM in a whole cell assay. A-620223 demonstrates good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with Temozolomide (TMZ) (HY-17364) and in an MX-1 breast xenograph model in combination with Cisplatin (HY-17394). A-620223 can be used for the studies of melanoma and breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 272769-49-0
- Formula: C16H22N4O
- Molecular Weight:286.37
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) A-620223
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Biological Activity
Description
IC50 & Target
[1]|
PARP-1 8 nM (Ki) |
Parmacokinetics
| Species | Dose | Route | Vss | F | CL | Cmax | AUC | T1/2 |
|---|---|---|---|---|---|---|---|---|
| Dog[1] | 4.1 mg/kg | p.o. | 3.6 L/kg | 82 % | 0.9 L/h/kg | 1 μg/mL | 3.7 μg·h/mL | / |
| Mice[1] | 10 mg/kg | p.o. | 9.1 L/kg | 63 % | 5.3 L/h/kg | 0.4 μg/mL | 1.2 μg·h/mL | / |
| Mice[1] | 3 mg/kg | i.v. | / | / | / | / | / | 1.2 h |
| Monkey[1] | 4.1 mg/kg | p.o. | 4.9 L/kg | 32 % | 2 L/h/kg | 0.2 μg/mL | 0.7 μg·h/mL | / |
| Rat[1] | 4.1 mg/kg | p.o. | 10.7 L/kg | 48 % | 2.9 L/h/kg | 0.8 μg/mL | 0.7 μg·h/mL | / |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B16F10 melanoma model and MX-1 breast cancer xenograft model established in C57BL/6 mice and female SCID mice[1]
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Dosage:1, 12.5 and 25 mg/kg (melanoma model); 5 and 25 mg/kg (breast cancer model)
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Administration:Subcutaneous injection (s.c.), successive administration for 7-14 days
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Result:Showed excellent potentiation of cytotoxic agents in two subcutaneous, murine tumor models.
Chemical Information
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CAS No. 272769-49-0
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Appearance Solid
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Molecular Weight 286.37
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Formula C16H22N4O
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SMILES
CCCN(CC1)CCC1C2=NC3=C(C(N)=O)C=CC=C3N2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Protocols
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How to Select the Route of Administration for Mammals
Route-of-administration selection in mammals is a pharmacokinetic, pharmacodynamic, formulation, animal-welfare, and translational decision, not a default technical choice. The selected route should match the study goal: intravenous dosing is most useful when complete systemic exposure and rapid onset are required, oral dosing is most translational for orally intended medicines but is affected by absorption and first-pass metabolism, subcutaneous or intramuscular dosing can provide slower systemic exposure, and intraperitoneal dosing can be useful in rodent proof-of-concept studies but may have limited clinical translation. Published route-comparison studies show that the same compound can produce different exposure, onset, bioavailability, tissue distribution, and tolerability depending on route; therefore, route choice should be supported by pilot pharmacokinetic or pharmacodynamic evidence when the literature is insufficient. Unresolved questions include how to standardize route sel
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
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Data Sheet (270 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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)