Tasquinimod | B2855

Tasquinimod has anti-angiogenic, antitumor and immune-modulatory properties. It shows consistent anti-angiogenic activity in vitro at doses between 10-50 μM. The mechanism of action of tasquinimod is not clear but may involve inhibition of MDSC action, a key immune checkpoint in cancer, inhibition of the hypoxia-induced angiogenic switch through epigenetic regulation of HDAC3/4 interactions, which may delay metastatic progression and engagement of the S100A9 protein. It is under clinical evaluation for use in combination therapy with other systemic agents in prostate cancer and as a single agent in solid tumors.

Tasquinimod has anti-angiogenic, antitumor and immune-modulatory properties. It shows consistent anti-angiogenic activity in vitro at doses between 10-50 μM. The mechanism of action of tasquinimod is not clear but may involve inhibition of MDSC action, a key immune checkpoint in cancer, inhibition of the hypoxia-induced angiogenic switch through epigenetic regulation of HDAC3/4 interactions, which may delay metastatic progression and engagement of the S100A9 protein. It is under clinical evaluation for use in combination therapy with other systemic agents in prostate cancer and as a single agent in solid tumors.

B2855 | Tasquinimod DataSheet

Alternate Name/Synonyms: 4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]quinoline-3-carboxamide; 1,2-dihydro-4-hydroxy-5-methoxy-N,1-dimethyl-2-oxo-N-[4-(trifluoromethyl)phenyl]-3-quinolinecarboxamide; N-Methyl-N-(4-trifluoromethyl-phenyl)-1,2-dihydro-4-hydroxy-5-methoxy-1-methyl-2-oxo-quinoline-3-carboxamide; ABR-215050

Appearance: A crystalline solid

Formulation:

CAS Number: 254964-60-8

Structure Available?: True

Peptide sequence:

Salt Form: false

Molecular Formula: C₂₀H₁₇F₃N₂O₄

Molecular Weight: 406.36

Cell-Permeable?: True

Purity: 99.85%

Solubilities: ~2 mg/ml in in Ethanol, ~10 mg/ml in in DMSO, ~20 mg/ml in DMF in 0

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A small molecule with anti-angiogenic, antitumor and immune-modulatory properties

MDL Number:

PubChem CID: 54682876

SMILES: CN1C2=C(C(=CC=C2)OC)C(=C(C1=O)C(=O)N(C)C3=CC=C(C=C3)C(F)(F)F)O

InChi: InChI=1S/C20H17F3N2O4/c1-24(12-9-7-11(8-10-12)20(21,22)23)18(27)16-17(26)15-13(25(2)19(16)28)5-4-6-14(15)29-3/h4-10,26H,1-3H3

InChi Key: ONDYALNGTUAJDX-UHFFFAOYSA-N