| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg | |||
| Other Sizes |
| Targets |
HIF-IN-1 targets Hypoxia-Inducible Factor-1 (HIF-1), specifically inhibiting the accumulation of the HIF-1alpha protein subunit.
|
|---|---|
| ln Vitro |
HIF-IN-1 potently inhibits HIF-1alpha protein aggregation. It demonstrates no obvious cell toxicity in vitro and does not affect HIF-1alpha mRNA levels, distinguishing it from transcriptional inhibitors.
|
| ln Vivo |
Dedicated in vivo activity studies for HIF-IN-1 are not extensively documented. However, as a HIF-1 inhibitor, it is hypothesized to disrupt cancer cell adaptation to hypoxia in animal models, potentially reducing tumor growth and metastasis.
|
| Enzyme Assay |
In vitro enzyme/receptor binding assays were conducted using cellular models to assess HIF-1alpha protein levels. Cells were treated with HIF-IN-1, followed by Western blotting to detect HIF-1alpha protein accumulation. mRNA levels were analyzed via qPCR to confirm the post-transcriptional mechanism of action.
|
| Cell Assay |
Cells were cultured and treated with varying concentrations of HIF-IN-1. Cell lysates were harvested, and HIF-1alpha protein levels were measured using Western blot analysis. Cytotoxicity was evaluated using standard assays such as MTT or Cell Counting Kit-8 (CCK-8) to confirm the compound does not induce cell death at effective concentrations.
|
| Animal Protocol |
In vivo protocols typically involve establishing tumor xenografts in immunodeficient mice (e.g., nude mice). Once tumors reach a specific size, animals are randomized into groups and administered HIF-IN-1 via intraperitoneal or oral routes. Tumor volumes and body weights are monitored regularly.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties for HIF-IN-1 are not fully documented in standard profiles. As a research compound with good solubility in DMSO, it is typically administered via intraperitoneal injection or other parenteral routes in preclinical studies.
|
| Toxicity/Toxicokinetics |
The primary safety profile of HIF-IN-1 indicates no obvious cell toxicity or cytotoxicity in vitro at effective concentrations. Comprehensive toxicological assessments, including acute and sub-chronic toxicity studies in animal models, have not been widely reported for this specific compound.
|
| References | |
| Additional Infomation |
The compound is designated as Compound 3c in the original research. Its mechanism of action is distinct from other HIF inhibitors as it suppresses HIF-1alpha protein aggregation rather than inhibiting its transcription or promoting its degradation via the proteasome. It is strictly for research use and is not an approved clinical drug.
|
| Molecular Formula |
C17H12N2O
|
|---|---|
| Molecular Weight |
260.28998374939
|
| Exact Mass |
260.094
|
| CAS # |
2393928-76-0
|
| PubChem CID |
156014427
|
| Appearance |
Yellow to orange solid powder
|
| LogP |
3.7
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
20
|
| Complexity |
389
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N1=CC2C3=C(C=CC=C3)C(=O)C=2N1C1=CC=C(C)C=C1
|
| InChi Key |
ZMPVOQJDQIWRJZ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H12N2O/c1-11-6-8-12(9-7-11)19-16-15(10-18-19)13-4-2-3-5-14(13)17(16)20/h2-10H,1H3
|
| Chemical Name |
3-(4-methylphenyl)indeno[2,1-c]pyrazol-4-one
|
| 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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~10 mg/mL (~38.42 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8419 mL | 19.2093 mL | 38.4187 mL | |
| 5 mM | 0.7684 mL | 3.8419 mL | 7.6837 mL | |
| 10 mM | 0.3842 mL | 1.9209 mL | 3.8419 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.
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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
