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| Size | Price | Stock |
|---|---|---|
| 250mg | $1500 | Check With Us |
| 500mg | $2250 | Check With Us |
| 1g | $3375 | Check With Us |
: Cat #: V13346 CAS #: 1672662-14-4 Purity ≥ 99%
Description: PT2399 is a novel, potent, and orally bioavailable small molecule inhibitor of HIF-2 which binds to HIF-2α PAS B domain with an IC50 of 6 nM, exhibiting potent antitumor activity in vivo.. It selectively disrupts the heterodimerization of HIF-2α with HIF-1β. Preclinical and clinical data indicate that PT2399 is effective in blocking cancer cell growth, proliferation, and tumor angiogenesis characteristic in ccRCC.
References: [1]. Chen W, et al. Targeting renal cell carcinoma with a HIF-2 antagonist. Nature. 2016 Nov 3;539(7627):112-117.
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| Molecular Weight (MW) | 419.322 |
|---|---|
| Molecular Formula | C17H10F5NO4S |
| CAS No. | 1672662-14-4 |
| SMILES Code | N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C(F)F)=O)C3=C2CC(F)(F)[C@H]3O)=C1 |
| Synonyms | PT2399; PT-2399; PT 2399 |
| Protocol | 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. | |
| Animal model | Mice with RCC tumorgraft | |
| Dosages | 100 mg/kg | |
| Administration | Oral gavage; every 12 hours |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.3848 mL | 11.9240 mL | 23.8480 mL | 47.6960 mL |
| 5mM | 0.4770 mL | 2.3848 mL | 4.7696 mL | 9.5392 mL |
| 10mM | 0.2385 mL | 1.1924 mL | 2.3848 mL | 4.7696 mL |
| 20mM | 0.1192 mL | 0.5962 mL | 1.1924 mL | 2.3848 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.