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Belzutifan

  Cat. No.:  DC72867  
Chemical Structure
For research use only. We do not sell to patients.
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More than 5000 active chemicals with high quality for research!
Field of application
Belzutifan (PT2977, MK-6482) is a potent and selective small-molecule inhibitor of HIF2α with SPA IC50 of 9 nM, EC50 of 11 nM (HIF-2α luciferase assay). PT2977 demonstrated high potency with EC50 of 17 nM in the VEGFA secretion assay in 786-O cells. PT2977 (0.3, 1, and 3 mg/kg, oral) potently and dose-dependently reduced mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, exhibited excellent antitumor activity in the 786-O mouse xenograft model In phase 1 clinical, PT2977 decreased in the HIF-2α target erythropoietin (EPO) following once daily oral administration of PT2977 at the dose levels of 20, 40, 80, 120, 160, and 240 mg in patients with solid tumors, also showed encouraging outcomes in patients with advanced renal cell carcinoma in an expansion cohort of 55 patients with ccRCC treated at 120 mg q.d.
Cas No.:
Chemical Name: Belzutifan
Formula: C17H12F3NO4S
M.Wt: 383.341
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
Cat. No. Product name Field of application
DC77009 ISM012-042 ISM012-042 is an orally active PHD1 and PHD2 inhibitor with IC50 values of 1.9 and 2.5 nM, respectively. ISM012-042 (2.5 μM) can protect Caco-2 cells from DSS-induced barrier disruption. In lipopolysaccharide (LPS)-induced mouse bone marrow-derived dendritic cells (BMDC), ISM012-042 has anti-inflammatory effects and can dose-dependently reduce the expression of IL-12 subunit IL-12p35 and TNF. ISM012-042 restores intestinal barrier function and alleviates intestinal inflammation in various experimental colitis models. ISM012-042 can be used for intestinal mucosal repair and research into immune diseases.
DC48260 Izilendustat Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1).
DC47980 HIF-2α-IN-4 HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing.
DC41030 1,4-DPCA ethyl ester 1,4-DPCA ethyl ester is the ethyl ester of 1,4-DPCA and can inhibit factor inhibiting HIF (FIH).
DC10436 SYP-5 SYP-5 is a novel HIF-1 inhibitor, suppresses tumor cells invasion and angiogenesis.
DC9811 PT2399 PT2399(PT=2399) is a novel HIF2α Antagonist.
DC11782 IDF-11774 IDF-11774 is a novel hypoxia-inducible factor α (HIFα)-1 inhibitor with an IC50 of 3.65 μM.
DC11607 JTZ-951(Enarodustat) A novel potent, orally active HIF prolyl hydroxylase (PHD) inhibitor with IC50 of 0.22 uM for PHD2.
DC77012 Octyl-α-ketoglutarate Octyl-α-ketoglutarate (1-Octyl 2-oxopentanedioate) is a stable, cell-permeable form of α-ketoglutarate which accumulates rapidly in HEK293 cells with a dysfunctional tricarboxylic acid (TCA) cycle, stimulating prolyl hydroxylase (PHD) activity. In addition, Octyl-α-ketoglutarate competitively blocks succinate- or fumarate-mediated inhibition of PHD.
DC77011 LW1564 LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model.
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