Description
Key facts
CAS number:1672665-49-4,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:383.3 Da,
Molecular formula:C17H12F3NO4S,
PubChem:91754484,
Nature:Synthetic,
Solubility:DMSO,
Biochemical name:3-{[(1s)-2,2-Difluoro-1-Hydroxy-7-(Methylsulfonyl)-2,3-Dihydro-1h-Inden-4-Yl]oxy}-5-Fluorobenzonitrile,
Biological description:Potent and selective inhibitor of hypoxia inducible factor (HIF-2α) with potential antineoplastic activity. PT-2385 selectively disrupts the heterodimerization of HIF-2α with HIF-1β. Very effective in blocking cancer cell growth, proliferation, and tumor angiogenesis in clear cell renal cell carcinoma (ccRCC).,
Canonical smiles:CS(=O)(=O)C1=C2C(C(CC2=C(C=C1)OC3=CC(=CC(=C3)C#N)F)(F)F)O,
Isomeric smiles:CS(=O)(=O)C1=C2[C@@H](C(CC2=C(C=C1)OC3=CC(=CC(=C3)C#N)F)(F)F)O,
InChi:InChI=1S/C17H12F3NO4S/c1-26(23,24)14-3-2-13(12-7-17(19,20)16(22)15(12)14)25-11-5-9(8-21)4-10(18)6-11/h2-6,16,22H,7H2,1H3/t16-/m0/s1,
InChiKey:ONBSHRSJOPSEGS-INIZCTEOSA-N,
IUPAC Name:3-[[(1S)-2,2-difluoro-1-hydroxy-7-methylsulfonyl-1,3-dihydroinden-4-yl]oxy]-5-fluorobenzonitrile
Product details:
This product is manufactured by BioVision, an Abcam company and was previously called B1920 PT-2385. B1920-5 is the same size as the 5 mg size of ab235501.
Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-It is important to note that this is air sensitive and impurities can occur as a result of air oxidation, Store in the dark, Store under desiccating conditions
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
HIF-2-alpha also known as EPAS1 is a transcription factor that plays a central role in response to oxygen levels in cells. HIF-2-alpha has a molecular weight of approximately 118 kDa. It is found in various tissues but is mainly expressed in endothelial cells lung and heart tissues. During hypoxic conditions it interacts with HIF-1-beta to initiate transcription of genes that promote oxygen homeostasis. Cytochrome P450 2C9 and Cytochrome P450 2C19 are enzymes involved in drug metabolism. CYP2C9 has a molecular weight of about 55.9 kDa and CYP2C19 has a molecular weight of about 56.4 kDa. Both are found in the liver and to a lesser extent in the small intestine.
Biological function summary
HIF-2-alpha regulates genes that are important for angiogenesis erythropoiesis and metabolic adaptation to low oxygen. It is part of the hypoxia-inducible factor (HIF) complex alongside HIF-1-alpha and HIF-1-beta. Meanwhile CYP2C9 and CYP2C19 help metabolize various drugs and activate prodrugs through oxidation reactions. They contribute to the clearance of substances from the body and the synthesis of cholesterol steroids and other lipids. Both enzymes play roles in the metabolism of endogenous and exogenous compounds.
Pathways
HIF-2-alpha is significant in the hypoxia pathway where it regulates gene expression to adapt to low oxygen levels. It associates with proteins like VEGF which promote new blood vessel formation. CYP2C9 and CYP2C19 are integral to the drug metabolism pathway specifically the cytochrome P450-dependent oxidation. They interact with proteins such as NADPH-cytochrome P450 reductase to perform their enzymatic activities.
HIF-2-alpha is implicated in cancer where its overexpression contributes to tumor growth and metastasis by promoting angiogenesis. It interacts with proteins like VEGF in this context. CYP2C9 and CYP2C19 are related to adverse drug reactions and disorders like Warfarin sensitivity and clopidogrel resistance respectively. Their interactions with various drugs can lead to altered drug efficacy and risk of toxicity in individuals with certain genetic polymorphisms.
