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2820286-56-2

2820286-56-2 Structure

2820286-56-2 Structure
IdentificationBack Directory
[Name]

Anticancer agent 81
[CAS]

2820286-56-2
[Synonyms]

Anticancer agent 81
[Molecular Formula]

C46H46N6O5
[MOL File]

2820286-56-2.mol
[Molecular Weight]

762.9
Chemical PropertiesBack Directory
[density ]

1.355±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
[pka]

7.682±0.10(predicted)
Hazard InformationBack Directory
[Uses]

Anticancer agent 81 (Compound 37b3) is an anticancer agent and can induce tumor cell cycle arrest and apoptosis. Anticancer agent 81 can be used as a payload to conjugate with Trastuzumab (HY-P9907) to obtain the antibody–agent conjugate (ADC) T-PBA. T-PBA maintained its mode of target and internalization ability of Trastuzumab[1].
[in vivo]

T-PBA (1-10 mg/kg; i.v.; every 3 days for 4 times) could significantly delay tumor growth in two Her2-positive xenograft models in mice without obvious toxicity and side effects, and the effect is better than Trastuzumab[1].

Animal Model:Female balb/c nude mice, SKOV3 and NCI-N87 tumor model[1]
Dosage:1, 5 and 10 mg/kg
Administration:Tail vein injection on days 0, 3, 6, and 9
Result:Inhibited tumor growth in a dose-dependent manner (57.5% inhibition at 1 mg/kg, 70.0% inhibition at 5 mg/kg, and 91.5% inhibition at 10 mg/kg in SKOV3 tumor model; the tumor growth inhibitory rate was 50.2% for 1 mg/kg, 88.0% for 5 mg/kg, and 97.1% for 10 mg/kg in NCI-N87 tumor model) without obvious side effects.
[References]

[1] Lai W, et al. Design, Synthesis, and Bioevaluation of a Novel Hybrid Molecular Pyrrolobenzodiazepine-Anthracenecarboxyimide as a Payload for Antibody-Drug Conjugate. J Med Chem. 2022 Aug 18. DOI:10.1021/acs.jmedchem.2c00471
2820286-56-2 suppliers list
Company Name: TargetMol Chemicals Inc.
Tel: +17819995354 , +17819995354
Website:
Company Name: TargetMol Chemicals Inc.  
Tel: 15002134094
Website: https://www.targetmol.cn/
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