BI-4142
Based on 1 Customer Validation
BI-4142 is a potent, highly selective and orally active HER2 inhibitor with an IC50 of 5 nM.
For research use only. We do not sell to patients.
- Purity: 98.02%
- CAS No.: 2682003-36-5
- Formula: C28H27N9O2
- Molecular Weight:521.57
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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HER2 5 nM (IC50) |
BI-4142 shows inhibition with IC50 values of 10 nM, 18 nM, 270 nM and 2400 nM against HEK HER2YVMA, Ba/F3 HER2YVMA, HEK EGFRWT and Ba/F3 EGFRWT, respectively[1].
BI-4142 (1 nM-5 μM, 72 h or 96 h) shows antiproliferative activity against tumor cells[1].
BI-4142 displays good permeability and no PgP-mediated efflux liability in the CaCo-2 assay[1].
BI-4142 inhibits HER2-dependent cell lines and inhibits downstream signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H2170 HER2WT, NCI-H2170 HER2YVMA, A431 EGFRWT, Ba/F3 HER2YVMA, Ba/F3 HER2YVMA,S783C, Ba/F3 EGFRWT and Ba/F3 EGFRC775S cells
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Concentration:1 nM-5 μM
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Incubation Time:72 h or 96 h
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Result:Showed antiproliferative effect with IC50 values of 16 nM, 82 nM, >5 µM, 4 nM, 24 nM, 718 nM and 43 nM against NCI-H2170 HER2WT, NCI-H2170 HER2YVMA, A431 EGFRWT, Ba/F3 HER2YVMA, Ba/F3 HER2YVMA,S783C, Ba/F3 EGFRWT and Ba/F3 EGFRC775S, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NMRI-Foxn1nu mice, PC-9 HER2YVMA xenograft model[1]
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Dosage:3, 10, 30 and 100 mg/kg
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Administration:Oral administration, twice per day for 40 days
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Result:Resulted in tumor regressions in a dose-dependent manner (113%, 126%, 153% and 166% tumor growth inhibition at 3, 10, 30 and 100 mg/kg, respectively).
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Animal Model:BomTac:NMRI Foxn1nu mice[1]
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Dosage:1 mg/kg or 10mg/kg and 100 mg/kg
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Administration:IV for 1 mg/kg, PO for 10mg/kg and 100 mg/kg (Pharmacokinetic Analysis)
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Result:In vivo mouse PK data for BI-4142[1]
Compound Dose iv/po
(mg/kg)tmax
(h)Cmax
(nM)AUD
(h•nM)Plasma CL
(mL/min/kg)% F i.v., 1mg/kg n/a n/a 3,280 9.69 n/a BI-4142 p.o., 10 mg/kg 0.83 8,600 23,200 n/a 71 p.o., 100 mg/kg 0.67 36,400 196,000 n/a 60
Chemical Information
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CAS No. 2682003-36-5
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Appearance Solid
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Molecular Weight 521.57
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Formula C28H27N9O2
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Color Light yellow to yellow
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SMILES
O=C(N1CCN(CC1)C2=NC=C3N=CN=C(C3=N2)NC4=CC=C(C(C)=C4)OC5=CC(N=CN6C)=C6C=C5)C=C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (191.73 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 (protect from light). 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 (protect from light). 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 (4.79 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 (4.79 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (protect from light)
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.
Purity & Documentation
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Data Sheet (277 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 (protect from light). 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 | 1.9173 mL | 9.5864 mL | 19.1729 mL | 47.9322 mL |
| 5 mM | 0.3835 mL | 1.9173 mL | 3.8346 mL | 9.5864 mL | |
| 10 mM | 0.1917 mL | 0.9586 mL | 1.9173 mL | 4.7932 mL | |
| 15 mM | 0.1278 mL | 0.6391 mL | 1.2782 mL | 3.1955 mL | |
| 20 mM | 0.0959 mL | 0.4793 mL | 0.9586 mL | 2.3966 mL | |
| 25 mM | 0.0767 mL | 0.3835 mL | 0.7669 mL | 1.9173 mL | |
| 30 mM | 0.0639 mL | 0.3195 mL | 0.6391 mL | 1.5977 mL | |
| 40 mM | 0.0479 mL | 0.2397 mL | 0.4793 mL | 1.1983 mL | |
| 50 mM | 0.0383 mL | 0.1917 mL | 0.3835 mL | 0.9586 mL | |
| 60 mM | 0.0320 mL | 0.1598 mL | 0.3195 mL | 0.7989 mL | |
| 80 mM | 0.0240 mL | 0.1198 mL | 0.2397 mL | 0.5992 mL | |
| 100 mM | 0.0192 mL | 0.0959 mL | 0.1917 mL | 0.4793 mL |
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