| Chemical Properties | Back Directory | [density ]
1.38±0.1 g/cm3(Predicted) | [solubility ]
DMSO: Sparingly soluble: 1-10 mg/ml | [form ]
Solid | [pka]
5.33±0.10(Predicted) | [color ]
Light yellow to yellow | [InChIKey]
PHDAGSZQGNWGFE-FKEMPHOKNA-N | [SMILES]
CC1=C(C(C)=NC2=NC(C)=NN12)O[C@@H]1CCN(C2C=CC(C3N=NC(CN4CCOCC4)=CC=3)=CC=2)C1 |&1:13,r| |
| Hazard Information | Back Directory | [Description]
AZD0095 is a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology. AZD0095 has excellent potency (1.3 nM), MCT1 selectivity (>1000×), secondary pharmacology, clean mechanism of action, suitable properties for oral administration in the clinic, and good preclinical efficacy in combination with cediranib. | [Uses]
AZD0095 is a selective and orally active MCT4 inhibitor (IC50: 1.3 nM). AZD0095 effectively inhibits the tumor growth in NCI-H358 xenograft in combination with Cediranib (HY-10205)[1]. | [in vivo]
AZD0095 (100 mg/kg, p.o. bid) together with Cediranib (3 mg/kg, p.o.) reduces tumor growth in a murine NCI-H358 xenograft[1].
| Animal Model: | Murine NCI-H358 xenograft[1] | | Dosage: | 100 mg/kg together with Cediranib (3 mg/kg) | | Administration: | Oral administration (p.o.) | | Result: | Reduced tumor growth more efficiently than AZD0095 or AZD2171 alone. |
| [IC 50]
MCT4: 1.3 nM (IC50) | [References]
[1] Goldberg FW, et al. Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology. J Med Chem. 2022 Dec 16. DOI:10.1021/acs.jmedchem.2c01342 |
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| Company Name: |
Bide Pharmatech Ltd.
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| Telephone: |
400-1647117 13681763483 |
| Website: |
https://www.bidepharm.com/ |
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