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PT2399

CAS No. : 1672662-14-4

產(chǎn)品活性：PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC₅₀ of 6 nM. PT2399 displays potent antitumor activity in vivo.

研究領(lǐng)域：Metabolic Enzyme/Protease

作用靶點(diǎn)：HIF/HIF Prolyl-Hydroxylase

In Vitro: PT2399 (compound 10f) inhibits HIF-2α with an IC₅₀ of 6 nM.
PT2399 can bind directly to the HIF-2α PAS B domain, and cripple HIF-2α’s ability to bind to Aryl hydrocarbon receptor nuclear translocator (ARNT).
PT2399 (20 μM) causes off-target toxicity because it inhibits the proliferation of HIF-2α ?/? 786-O cells and other cancer cell lines with undetectable HIF-2α.
PT2399 (0.2–2 μM; 0-21 days) inhibits 786-O cells soft agar growth.
PT2399 represses various HIF target genes in 786-O VHL?/? ccRCC cells, does not suppress HIF-1α-specific targets such as BNIP3.

In Vivo: PT2399 inhibits tumor cell proliferation 3.5 fold in renal cell carcinoma (RCC) bearing mice.
PT2399 reduces tumor cell density and increases fibrosis in RCC bearing mice.
PT2399 (100 mg/kg; oral gavage; every 12 hours) is more active than SU 11248, and inhibits tumor growth in several SU 11248-resistant tumors in RCC bearing mice .
PT2399 directly inhibits HIF-2α causes tumor regression in preclinical models of primary and metastatic pVHL-defective ccRCC in an on-target fashion.

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