HIF-2α-IN-18
HIF-2α-IN-18 is a selective HIF-2α inhibitor with a human IC50 of 8.1 nM. HIF-2α-IN-18 binds to the HIF-2α PAS-B domain, induces conformational perturbations at the HIF-2α/ARNT dimerization interface, destabilizes the HIF-2α/ARNT heterodimer, and blocks HIF-2α-mediated transcriptional activity. HIF-2α-IN-18 inhibits hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1, without inhibiting HIF-1α target genes PGK1 and PDK1. HIF-2α-IN-18 can be used for the research of clear cell renal cell carcinoma, hepatocellular carcinoma[1].
For research use only. We do not sell to patients.
- CAS No.: 2709068-47-1
- Formula: C18H8F7N3
- Molecular Weight:399.27
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
|
HIF-2α 8.1 nM (IC50) |
HIF-2α-IN-18 (Compound 13) (1 h; 45 min) potently inhibits binding to recombinant human HIF-2α PAS-B protein with an SPA IC50 of 14.8 nM[1].
HIF-2α-IN-18 (20 h) potently inhibits HIF-2α-mediated transcriptional activity in 786-O ccRCC cells with a cellular luciferase IC50 of 8.1 nM[1].
HIF-2α-IN-18 (20 h) inhibits HIF-2α-mediated transcriptional activity in 786-O ccRCC cells in 100% human serum with a cellular luciferase IC50 of 0.82 μM[1].
HIF-2α-IN-18 (0-50 μM; 20 h) inhibits HIF-2α-regulated VEGF-A secretion in 786-O ccRCC cells with an IC50 of 60 nM[1].
HIF-2α-IN-18 (0.01-10 μM; 20 h) potently and selectively inhibits hypoxia-induced HIF-2α target gene (EPO, SERPINE1) expression in Hep3B hepatocellular carcinoma cells without inhibiting HIF-1α target gene (PGK1, PDK1) expression[1].
HIF-2α-IN-18 (0.5 μM) has an in vitro intrinsic clearance of 29.2 μL/min/106 cells in human hepatocytes and 141 μL/min/106 cells in rat hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Hep3B hepatocellular carcinoma cells (intact VHL, functional HIF-1α and HIF-2α)
-
Concentration:0.01 μM; 0.1 μM; 10 μM
-
Incubation Time:20 h
-
Result:Dose-dependently inhibited hypoxia-induced expression of HIF-2α target genes EPO and SERPINE1.
No robust or dose-dependent inhibition of HIF-1α target genes PGK1 and PDK1 was observed.
Maintained cell viability throughout the assay.
| Species | Dose | Route | CL | Vss | T1/2 | MRTINF_obs |
|---|---|---|---|---|---|---|
| Rat[1] | 0.25 mg/kg | i.v. | 6.31 L/h/kg | 9.60 L/kg | 2.15 h | 1.53 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Sprague-Dawley (male, weight 200-250 g)[1]
-
Dosage:0.25 mg/kg
-
Administration:i.v.; single dose
-
Result:Achieved an in vivo clearance (CL) of 6.31 L/h/kg.
Reached a volume of distribution at steady state (Vss) of 9.60 L/kg.
Had an elimination half-life (T1/2) of 2.15 h.
Exhibited a mean residence time (MRTINF) of 1.53 h.
Showed plasma protein binding (PPB) of 93.1% bound.
Chemical Information
-
CAS No. 2709068-47-1
-
Molecular Weight 399.27
-
Formula C18H8F7N3
-
SMILES
F[C@@H]1C(C=C(F)C=C2C#N)=C2N(C3=CC=C(C(F)(F)F)C(F)=C3C#N)C[C@@H]1F
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HIF-2α-IN-18 Related Classifications
HY-183583 Related Classifications
Powered by Bioz