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HIF-1α-IN-2

Cat No.:V50171 Purity: ≥98%
HIF-1α-IN-2 is a potent HIF-1α inhibitor (antagonist) with anti-cancer effects, with IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively.
HIF-1α-IN-2
HIF-1α-IN-2 Chemical Structure CAS No.: 2762315-06-8
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
HIF-1α-IN-2 is a potent HIF-1α inhibitor (antagonist) with anti-cancer effects, with IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively. HIF-1α-IN-2 inhibits HIF-1α expression by blocking transcription and inhibiting protein translation.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
HIF-1α-IN-2 (compound 7f) reduces MDA-MB-231 and MiaPaCa-2 cell survival at 5 μM and 72 hours, respectively, with IC50 values of 28 nM and 15 nM [1]. With a dose-dependent impact, HIF-1α-IN-2 (0.25, 0.5, and 1 µM; 16–24h) can considerably (0–1 µM; 72h) decrease the expression of HIF-1α and VEGF [1]. inhibited the migration of MDA-MD-231 cells at concentrations of 56%, 0.25 µM, 83%, 0.5 µM, and 85%, 1 µM. It was also detected in MiaPaCa-2 cells. This indicates that HIF-1α- HIF-1α-IN-2 (0-1 μM; 72h) suppresses the levels of HIF-1α mRNA in MDA-MB-231 cells when they are hypoxic [1]. The anti-migration action of IN-2 is distinct [1]. viability test
Cell Assay
Viability assay
Cell Types: MDA-MB-231 cells, MiaPaCa-2 cells [1]
Tested Concentrations: 5 μM
Incubation Duration: 72 hrs (hours)
Experimental Results: Inhibited the viability of these two cell lines, the IC50 in MDA-MB was 28 nM respectively and 15 nM for -231 and MiaPaCa-2 cells, respectively.

Cell viability assay
Cell Types: MDA-MB-231 cells, MiaPaCa-2 cells [1]
Tested Concentrations: 5 μM
Incubation Duration: 72 hrs (hours)
Experimental Results: Inhibited the viability of these two cell lines, the IC50 in MDA- was 28 nM and 15 nM for MB-231 and MiaPaCa-2 cells respectively.
References

[1]. Synthesis and evaluation of biarylquinoline derivatives as novel HIF-1α inhibitors. Bioorg Chem. 2022;121:105681.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H19N3OS
Molecular Weight
361.46
Exact Mass
361.124
CAS #
2762315-06-8
PubChem CID
163196195
Appearance
Off-white to light yellow solid powder
LogP
5.2
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
4
Heavy Atom Count
26
Complexity
465
Defined Atom Stereocenter Count
0
SMILES
N1C2C(=CC=C(OC)C=2)C(NC2=CC=CC(C3=CSC(C)=N3)=C2)=CC=1C
InChi Key
ILYYBJSTMKDZND-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H19N3OS/c1-13-9-19(18-8-7-17(25-3)11-20(18)22-13)24-16-6-4-5-15(10-16)21-12-26-14(2)23-21/h4-12H,1-3H3,(H,22,24)
Chemical Name
7-methoxy-2-methyl-N-[3-(2-methyl-1,3-thiazol-4-yl)phenyl]quinolin-4-amine
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~25 mg/mL (~69.16 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.92 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.7666 mL 13.8328 mL 27.6656 mL
5 mM 0.5533 mL 2.7666 mL 5.5331 mL
10 mM 0.2767 mL 1.3833 mL 2.7666 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(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.

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