AZD-5305
- Product Name
- AZD-5305
- CAS No.
- 2589531-76-8
- Chemical Name
- AZD-5305
- Synonyms
- AZD-5305;saruparib;AZD5305 ，S9875;Saruparib (AZD5305);AZD5305, 10 mM in DMSO;5-[4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methylpicolinamide;5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)-N-methylpicolinamide;5-{4-[(7-ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide;2-Pyridinecarboxamide, 5-[4-[(7-ethyl-5,6-dihydro-6-oxo-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methyl-;repair,AZD5305,Inhibitor,poly ADP ribose polymerase,DNA,AZD-5305,PARP,inhibit,pathway,synthetic,AZD 5305,lethality
- CBNumber
- CB58941287
- Molecular Formula
- C22H26N6O2
- Formula Weight
- 406.48
- MOL File
- 2589531-76-8.mol
AZD-5305 Property
- Boiling point:
- 702.6±60.0 °C(Predicted)
- Density
- 1.246±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 41.67 mg/mL (102.51 mM; Need ultrasonic)
- pka
- 11.26±0.40(Predicted)
- form
- Solid
- color
- Off-white to light yellow
- InChIKey
- WQAVGRAETZEADU-UHFFFAOYSA-N
- SMILES
- C1(C(NC)=O)=NC=C(N2CCN(CC3=CC4=C(N=C3)C=C(CC)C(=O)N4)CC2)C=C1
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P270Do not eat, drink or smoke when using this product.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P330Rinse mouth.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
AZD-5305 Chemical Properties,Usage,Production
Uses
Saruparib (AZD5305) is a potent, orally active and selective PARP inhibitor and trapper with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively. Saruparib has anti-proliferative activity and inhibits growth in cells with deficiencies in DNA repair[1][2].
in vivo
Saruparib (AZD5305) (0.01-0.3 mg/kg; p.o.; daily, for 35 d; female Han Wistar rats) demonstrates sustained antitumor activity in BRCAm xenograft and PDX models in vivo[1].
| Animal Model: | Female Han Wistar rats with BRCAm xenograft and PDX models (12-13 weeks of age)[1] |
| Dosage: | 0.01, 0.03, 0.1, and 0.3 mg/kg |
| Administration: | Oral administration; daily, for 35 days |
| Result: | Had antitumor efficacy in a dose-dependent manner. |
IC 50
PARP1: 3 nM (IC50); PARP2: 1400 nM (IC50)
References
[1] Illuzzi G, et, al. Preclinical Characterization of AZD5305, A Next-Generation, Highly Selective PARP1 Inhibitor and Trapper. Clin Cancer Res. 2022 Nov 1;28(21):4724-4736. DOI:10.1158/1078-0432.CCR-22-0301
[2] Johannes JW, et, al. Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs. J Med Chem. 2021 Oct 14;64(19):14498-14512. DOI:10.1021/acs.jmedchem.1c01012
AZD-5305 Preparation Products And Raw materials
Raw materials
Preparation Products
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