JNJ28871063 hydrochloride
Based on 1 Customer Validation
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.
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- Purity: 98.36%
- CAS No.: 944342-90-9
- 화학식: C24H28Cl2N6O3
- 분자량:519.42
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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ErbB1 22 nM (IC50) |
ErbB2 38 nM (IC50) |
ErbB4 21 nM (IC50) |
JNJ-28871063 demonstrates potent growth inhibition in vitro of human cancer cell lines (N87; BT474; SKBR3; A431; HN5) overexpressing the ErbB2 receptor with IC50 values with 60-168 nM. 28871063 exhibited the least effect at inhibiting growth of non–ErbB-over-expressing cell lines (HeLa, A375, HCT116, HT29, MRC5 primary fibroblasts cells; IC50>10 μM)[1].
JNJ-28871063 hydrochloride (3 μM; 16 hours) reduces the basal level of ErbB2 phosphorylation in SKBR3 cells[1].
JNJ28871063 hydrochloride is from an aminopyrimidine oxime structural class[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BT474 cells
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Concentration:3 μM
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Incubation Time:16 hours
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Result:Reduced the basal level of ErbB2 phosphorylation.
JNJ28871063 hydrochloride produces a significant inhibition of tumor growth at 100 mg/kg (TGI=66.8%) in an A431 human tumor xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude mice bearing N87 tumor xenografts[1]
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Dosage:100 mg/kg
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Administration:Oral; daily for 30 days
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Result:Showed significant inhibition of tumor growth (TGI=71%).
Chemical Information
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CAS No. 944342-90-9
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Appearance Solid
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분자량 519.42
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화학식 C24H28Cl2N6O3
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Color Light yellow to yellow
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SMILES
NC1=C(/C=N/OCCN2CCOCC2)C(NC3=CC(Cl)=C(OCC4=CC=CC=C4)C=C3)=NC=N1.Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 100 mg/mL (192.52 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (4.81 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.81 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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 | 1.9252 mL | 9.6261 mL | 19.2522 mL | 48.1306 mL |
| 5 mM | 0.3850 mL | 1.9252 mL | 3.8504 mL | 9.6261 mL | |
| 10 mM | 0.1925 mL | 0.9626 mL | 1.9252 mL | 4.8131 mL | |
| 15 mM | 0.1283 mL | 0.6417 mL | 1.2835 mL | 3.2087 mL | |
| 20 mM | 0.0963 mL | 0.4813 mL | 0.9626 mL | 2.4065 mL | |
| 25 mM | 0.0770 mL | 0.3850 mL | 0.7701 mL | 1.9252 mL | |
| 30 mM | 0.0642 mL | 0.3209 mL | 0.6417 mL | 1.6044 mL | |
| 40 mM | 0.0481 mL | 0.2407 mL | 0.4813 mL | 1.2033 mL | |
| 50 mM | 0.0385 mL | 0.1925 mL | 0.3850 mL | 0.9626 mL | |
| 60 mM | 0.0321 mL | 0.1604 mL | 0.3209 mL | 0.8022 mL | |
| 80 mM | 0.0241 mL | 0.1203 mL | 0.2407 mL | 0.6016 mL | |
| 100 mM | 0.0193 mL | 0.0963 mL | 0.1925 mL | 0.4813 mL |
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