Product Details
| Product Name:
PT2399 |
CAS No.:
1672662-14-4 |
| Purity:
99.07% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | PT2399 |
| 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 |
| 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]. |
| Storage | store 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)
|
| Keywords | Hypoxia-inducible factors | Inhibitor | PT2399 | PT-2399 | inhibit | HIF-PH | HIF/HIF Prolyl-Hydroxylase | HIFs | PT 2399 |
| Inhibitors Related | Deferoxamine Mesylate | Hydralazine hydrochloride | 1,4-DPCA | Chlorogenic Acid | Glucosamine | Hydroxycitric acid tripotassium hydrate | Glucosamine hydrochloride | Minocycline hydrochloride | Oltipraz | Acriflavine Hydrochloride | Glucosamine sulfate | Cinnamaldehyde |
| Related Compound Libraries | Glycolysis Compound Library | Reprogramming Compound Library | Bioactive Compound Library | HIF-1 Signaling Pathway Compound Library | Glutamine Metabolism Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$100.00/1mg |
VIP5Y
|
TargetMol Chemicals Inc.
|
2024-11-19 |
United States