WHI-P180
Based on 1 publication(s) in Google Scholar
WHI-P180 (Janex 3) is a multi-kinase inhibitor; inhibits RET, KDR and EGFR with IC50s of 5 nM, 66 nM and 4 μM, respectively.
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- Purity: 99.84%
- CAS No.: 211555-08-7
- 화학식: C16H15N3O3
- 분자량:297.31
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) WHI-P180
MoreAll VEGFR Isoforms
MoreAll EGFR Isoforms
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Biological Activity
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EGFR 4 μM (IC50) |
KDR 66 nM (IC50) |
RET 5 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
380 nM
Compound: 6
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Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay
Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay
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[PMID: 26874741] |
| BaF3 | IC50 |
890 nM
Compound: 6
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Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay
Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay
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[PMID: 26874741] |
| BaF3 | IC50 |
>10000 nM
Compound: 6
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Cytotoxicity in mouse BA/F3 cells after 48 hrs by Cell titre glo-based luminescence assay
Cytotoxicity in mouse BA/F3 cells after 48 hrs by Cell titre glo-based luminescence assay
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[PMID: 26874741] |
| HepG2 | IC50 |
18 μM
Compound: 9; WHI-P180
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Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation by MTT assay
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[PMID: 33460739] |
| MCF7 | IC50 |
24 μM
Compound: 9; WHI-P180
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Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation by MTT assay
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[PMID: 33460739] |
| Sf21 | IC50 |
66 nM
Compound: 6
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Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay
Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay
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[PMID: 26874741] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 211555-08-7
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Appearance Solid
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분자량 297.31
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화학식 C16H15N3O3
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Color White to off-white
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SMILES
COC1=CC2=NC=NC(NC3=CC=CC(O)=C3)=C2C=C1OC
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Synonyms
Janex 3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
용액&용해도
DMSO : 25 mg/mL (84.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (33.63 mM); Suspended solution; Need ultrasonic
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Inhibitors (WHI-P180) are pre-incubated in the plate for 15 min with 5 μL kinase and assay buffer at the following concentrations; 13 pM RET and 150 pM KDR. The reaction is initiated by the addition of 5 μL ATP and substrate at 2×final reaction concentrations. For RET, this is 18 μM and 2 μM; for KDR, this is 16 μM and 1 μM, respectively. Reactions are performed at ATP Km for each target. The assay is allowed to proceed at room temperature for 20 min before terminating with the addition of 10 μL HTRF detection buffer containing EDTA supplemented with TK-antibody labelled with Eu3+-Cryptate (1:100 dilution) and streptavidin-XL665 (128 nM). Following incubation at room temperature for 1 h, FRET signal is measured[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
IL3-dependent BaF3 cells are modified to express an activated recombinant kinase. Following removal of IL3, the modified cells are dependent on the activity of the recombinant kinase for survival and proliferation. The BaF3 cell lines, expressing KIF5B-RET and KDR are maintained in RPMI-1640 media containing 10% FBS and appropriate antibiotics. Non-modified BaF3 cells (WT) are maintained in RPMI-1640 media containing 10% FBS and supplemented with 10 ng/mL recombinant mouse IL3. For assessment of compound IC50, cells are plated into 384-well plates at 1500 or 3000 cells per well in 30 μL culture medium and compounds dispensed using an acoustic liquid handling platform. Following incubation of the cells for 48 h at 37 °C in a humidified 5% CO2 atmosphere, viability is determined by addition of 10 μL CellTiter-Glo reagent and measurement of luminescence[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: A high performance liquid chromatography (HPLC)-based quantitative detection method is used to measure plasma WHI-P180levels in mice. The plasma concentration-time data is fit to a single compartment pharmacokinetic model by using the WinNonlin program to calculate the pharmacokinetic parameters. A cutaneous anaphylaxis model is used to examine the pharmacodynamic effects of WHI-P180 on anaphylaxis-associated vascular hyperpermeability[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Newton R, et al. The discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity. Eur J Med Chem. 2016 Apr 13;112:20-32. [Content Brief]
[2]. Ghosh S, et al. 4-[3-Bromo-4-hydroxyphenyl)amino]-6,7-dimethoxyquinazolin-1-ium chloride methanol solvateand 4-[(3-hydroxyphenyl)amino]-6,7-dimethoxy-1-quinazolinium chloride. Acta Crystallogr C. 2001 Jan;57(Pt 1):76-8. [Content Brief]
[3]. Chen CL, et al. Pharmacokinetics and biologic activity of the novel mast cell inhibitor, 4-(3-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline in mice. Pharm Res. 1999 Jan;16(1):117-22. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3635 mL | 16.8175 mL | 33.6349 mL | 84.0873 mL |
| 5 mM | 0.6727 mL | 3.3635 mL | 6.7270 mL | 16.8175 mL | |
| 10 mM | 0.3363 mL | 1.6817 mL | 3.3635 mL | 8.4087 mL | |
| 15 mM | 0.2242 mL | 1.1212 mL | 2.2423 mL | 5.6058 mL | |
| 20 mM | 0.1682 mL | 0.8409 mL | 1.6817 mL | 4.2044 mL | |
| 25 mM | 0.1345 mL | 0.6727 mL | 1.3454 mL | 3.3635 mL | |
| 30 mM | 0.1121 mL | 0.5606 mL | 1.1212 mL | 2.8029 mL | |
| 40 mM | 0.0841 mL | 0.4204 mL | 0.8409 mL | 2.1022 mL | |
| 50 mM | 0.0673 mL | 0.3363 mL | 0.6727 mL | 1.6817 mL | |
| 60 mM | 0.0561 mL | 0.2803 mL | 0.5606 mL | 1.4015 mL | |
| 80 mM | 0.0420 mL | 0.2102 mL | 0.4204 mL | 1.0511 mL |
WHI-P180 Related Classifications
HY-15769 Related Classifications
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