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PT2399

Catalog No. T12675LCas No. 1672662-14-4

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

PT2399

PT2399

Purity: 99.07%
Catalog No. T12675LCas No. 1672662-14-4
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 SizePriceAvailabilityQuantity
1 mg$100In Stock
5 mg$247In Stock
10 mg$372In Stock
25 mg$673In Stock
50 mg$993In Stock
100 mg$1,390In Stock
1 mL x 10 mM (in DMSO)$272In Stock
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Purity:99.07%
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Product Introduction

Bioactivity
Description
PT2399 shows effective antitumor activity in vivo. PT2399 is an effective and selective HIF-2α antagonist, which directly binds to the HIF-2α PAS B domain (IC50: 6 nM).
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].
Chemical Properties
Molecular Weight419.32
FormulaC17H10F5NO4S
Cas No.1672662-14-4
Storage & Solubility Information
Storagestore at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 200 mg/mL (476.96 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3848 mL11.9241 mL23.8481 mL119.2407 mL
5 mM0.4770 mL2.3848 mL4.7696 mL23.8481 mL
10 mM0.2385 mL1.1924 mL2.3848 mL11.9241 mL
20 mM0.1192 mL0.5962 mL1.1924 mL5.9620 mL
50 mM0.0477 mL0.2385 mL0.4770 mL2.3848 mL
100 mM0.0238 mL0.1192 mL0.2385 mL1.1924 mL

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