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2217671-64-0

2217671-64-0 Structure

2217671-64-0 Structure
IdentificationBack Directory
[Name]

2-Propenoic acid, 3-[4'-[2-(hydroxyamino)-2-oxoethoxy]-3'-tricyclo[3.3.1.13,7]dec-1-yl[1,1'-biphenyl]-4-yl]-, (2E)-
[CAS]

2217671-64-0
[Synonyms]

MIR002
2-Propenoic acid, 3-[4'-[2-(hydroxyamino)-2-oxoethoxy]-3'-tricyclo[3.3.1.13,7]dec-1-yl[1,1'-biphenyl]-4-yl]-, (2E)-
[Molecular Formula]

C27H29NO5
[MOL File]

2217671-64-0.mol
[Molecular Weight]

447.52
Chemical PropertiesBack Directory
[density ]

1.303±0.06 g/cm3(Predicted)
[form ]

Solid
[pka]

4.49±0.10(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

MIR002 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. MIR002 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. MIR002 shows significant antitumor activity in vivo[1].
[in vivo]

MIR002 (50 mg/kg; p.o.; twice a day for 5 days a week, 3 weeks) shows a good tolerability and antitumor activity (TGI=61%)[1].
MIR002 (50 mg/kg; p.o.; twice a day for 5 days a week, 6 weeks) shows an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin[1].
MIR002 ( 50 mg/kg, twice a day for 5 days) induces a significant increase of a interferon at its pharmacological active dose (50 mg/kg)[1].

Animal Model:Model: 4-6 weeks old female CD-1 nude mice (NSCLC NCI-H460 model)
Dosage:50 mg/kg
Administration:p.o.; twice a day for 5 days a week, 3 weeks
Result:Showed a good tolerability and antitumor activity (TGI=61%).
Animal Model:4-6 weeks old female CD-1 nude mice ( MM473-luc and MM487-Luc)[1]
Dosage:50 mg/kg combibnated with cisplatin (i.p.; 5 mg/kg; twice a day for 7 days a week, 6 weeks)
Administration:p.o.; twice a day for 5 days a week, 6 weeks
Result:Showed an additive antitumor effect with complete disappearance of tumor masses in two animals at the end of the treatment when combination with cisplatin.
Animal Model:4-6 weeks old female CD-1 nude mice (Melanoma B16 model)[1]
Dosage:50 mg/kg
Administration:p.o.; twice a day for 5 days
Result:Induced a significant increase of α interferon at its pharmacological active dose (50 mg/kg).
[IC 50]

HDAC11: 6.09 μM (IC50); POLA1
[References]

[1] Dallavalle S, et al. Antitumor activity of novel POLA1-HDAC11 dual inhibitors. Eur J Med Chem. 2022, 228:113971. DOI:10.1016/j.ejmech.2021.113971
2217671-64-0 suppliers list
Company Name: TargetMol Chemicals Inc.
Tel: +17819995354 , +17819995354
Website:
Company Name: Shanghai Beckham Medical Technology Co., Ltd  
Tel: 021-13816613772 13816613772
Website: www.chemicalbook.com/ShowSupplierProductsList16976/0_EN.htm
Company Name: TargetMol Chemicals Inc.  
Tel: 15002134094
Website: https://www.targetmol.cn/
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