Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PT2399 is a first-in-class, orally available, small molecule inhibitor of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. PT2399 displays potent antitumor activity in vivo
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 121.00 | |
5 mg | In stock | $ 297.00 | |
10 mg | In stock | $ 396.00 | |
25 mg | In stock | $ 837.00 | |
50 mg | In stock | $ 1,160.00 | |
100 mg | In stock | $ 1,560.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 336.00 |
Description | PT2399 is a first-in-class, orally available, small molecule inhibitor of HIF-2 that selectively disrupts the heterodimerization of HIF-2α with HIF-1β. PT2399 displays potent antitumor activity in vivo |
Targets&IC50 | HIF2α:6 nM |
In vitro | PT2399, a selective HIF-2 antagonist that was identified using a structure-based design approach. PT2399 dissociated HIF-2 (an obligatory heterodimer of HIF-2α-HIF-1β) in human ccRCC cells and suppressed tumorigenesis in 56% (10 out of 18) of such lines[1].PT2399 inhibits HIF-2α (IC50: 6 nM). PT2399 represses various HIF target genes in 786-O VHL / ccRCC cells, does not suppress HIF-1α-specific targets such as BNIP3. PT2399 can cripple HIF-2α’s ability to bind to Aryl hydrocarbon receptor nuclear translocator (ARNT). PT2399 (20 μM) induces 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[2][3]. |
In vivo | PT2399) that directly inhibits HIF-2α causes tumour regression in preclinical mouse models of primary and metastatic pVHL-defective clear cell renal cell carcinoma in an on-target fashion[2].PT2399 inhibits tumor cell proliferation 3.5 fold in renal cell carcinoma (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.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 [1][2]. |
Molecular Weight | 419.32 |
Formula | C17H10F5NO4S |
CAS No. | 1672662-14-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 200 mg/mL (476.96 mM)
You can also refer to dose conversion for different animals. More
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PT2399 1672662-14-4 Angiogenesis Chromatin/Epigenetic Metabolism HIF/HIF Prolyl-Hydroxylase HIF Hypoxia-inducible factors Inhibitor PT-2399 inhibit HIF-PH HIFs PT 2399 inhibitor