1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. HIF-2α-IN-8

HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity.

For research use only. We do not sell to patients.

HIF-2α-IN-8 Chemical Structure

HIF-2α-IN-8 Chemical Structure

CAS No. : 2734922-78-0

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1 mg USD 300 In-stock
5 mg USD 880 In-stock
10 mg USD 1400 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity[1].

IC50 & Target

IC50: 9 nM (HIF2α SPA); 37 nM (HIF2α iScript); 246 nM (HIF2α HRE RGA)[1]

In Vivo

HIF-2α-IN-8 (Example 31) (30 mg/kg; p.o.; daily for 21 days) shows antitumor activity in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-9 weeks, female nude Crl:NU(NCr)-Foxn1nu-Homozygous mice (786-O mouse model)[1]
Dosage: 30 mg/kg
Administration: P.o.; started 34 days post tumor inoculation; daily for 21 days
Result: Inhibited the tumor growth.
Molecular Weight

441.73

Formula

C17H11ClF7N3O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1(C2=C(Cl)N=CC=C2[C@]3(CC1)N=C4N(C=C(C=C4OC(F)F)C(F)(F)F)C3)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (565.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2638 mL 11.3191 mL 22.6383 mL
5 mM 0.4528 mL 2.2638 mL 4.5277 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.85%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2638 mL 11.3191 mL 22.6383 mL 56.5957 mL
5 mM 0.4528 mL 2.2638 mL 4.5277 mL 11.3191 mL
10 mM 0.2264 mL 1.1319 mL 2.2638 mL 5.6596 mL
15 mM 0.1509 mL 0.7546 mL 1.5092 mL 3.7730 mL
20 mM 0.1132 mL 0.5660 mL 1.1319 mL 2.8298 mL
25 mM 0.0906 mL 0.4528 mL 0.9055 mL 2.2638 mL
30 mM 0.0755 mL 0.3773 mL 0.7546 mL 1.8865 mL
40 mM 0.0566 mL 0.2830 mL 0.5660 mL 1.4149 mL
50 mM 0.0453 mL 0.2264 mL 0.4528 mL 1.1319 mL
60 mM 0.0377 mL 0.1887 mL 0.3773 mL 0.9433 mL
80 mM 0.0283 mL 0.1415 mL 0.2830 mL 0.7074 mL
100 mM 0.0226 mL 0.1132 mL 0.2264 mL 0.5660 mL
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HIF-2α-IN-8 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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HIF-2α-IN-8
Cat. No.:
HY-148860
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