INDEX NAME NOT YET ASSIGNED
- CAS No.
- 2381268-71-7
- Chemical Name:
- INDEX NAME NOT YET ASSIGNED
- Synonyms
- OP-5244;OP5244,OP 5244
- CBNumber:
- CB98197639
- Molecular Formula:
- C19H29ClN5O9P
- Molecular Weight:
- 537.89
- MDL Number:
- MFCD34368525
- MOL File:
- 2381268-71-7.mol
INDEX NAME NOT YET ASSIGNED price
INDEX NAME NOT YET ASSIGNED Chemical Properties,Uses,Production
Uses
OP-5244 is a potent and orally active inhibitor of CD73, with an IC50 of 0.25 nM. OP-5244 reverses immunosuppression through blocking of adenosine production, and has the potential for the cancer research[1].
in vivo
OP-5244 (15 mg/kg/day; s.c. for 13 d) exhibits anti-tumor effects as a single agent as shown by the tumor growth inhibition in mice[1].
OP-5244 (150 mg/kg; p.o. twice daily for 16 d) increases CD8+ T cells infiltration and reverses immunosuppression in mice[1].
OP-5244 (0.2 mg/kg; i.v.) exhibits terminal elimination half-lives (rat 8.5, dog 0.82, cyno 4.6 h) due to moderate plasma clearance (rat 0.18, dog 1.22, cyno 0.05 L/kg/h) and low steady-state volume of distribution (rat 0.22, dog 0.29, cyno 0.10 L/kg/h)[1].
OP-5244 (10 mg/kg; p.o.) exhibits Cmax (rat 0.82, dog 1.25, cyno 1.72 μM) and AUC (rat 1.96, dog 1.75, cyno 14.2 μM h) [1].
Animal Model: | BALB/c mice with breast cancer[1] |
Dosage: | 15 mg/kg/day |
Administration: | S.c. for 13 days |
Result: | Inhibited tumor growth. Showed a 95% lower ADO/AMP ratio compared to that of the vehicle group. |
References
[1] Du X, et, al. Orally Bioavailable Small Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression Through Blockade of Adenosine Production. J Med Chem. 2020 Aug 31. DOI:10.1021/acs.jmedchem.0c01086
INDEX NAME NOT YET ASSIGNED Preparation Products And Raw materials
Raw materials
Preparation Products
INDEX NAME NOT YET ASSIGNED Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32239 | 58 |
Aladdin Scientific | tp@aladdinsci.com | United States | 52924 | 58 | |
ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3466 | 58 |
Chengdu DingDang Pharmaceutical Co., Ltd. | 028-86040038 13980902949; | market@dingdangchem.com | China | 1852 | 55 |
DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9409 | 58 |
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 021-59167510 18117107507 | vip@med-life.cn | China | 4997 | 58 |
RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9835 | 58 |