Falnidamol
Based on 4 publication(s) in Google Scholar
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
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- Pureza : 98.36%
- No. CAS: 196612-93-8
- Fòrmula: C18H19ClFN7
- Peso molecular:387.84
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Falnidamol
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
EGFR 3 nM (IC50) |
ErbB2 3.4 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KB | IC50 |
0.15 nM
Compound: K00619a, BIBX-1382
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Inhibition of EGF-mediated thymidine incorporation in human KB cells
Inhibition of EGF-mediated thymidine incorporation in human KB cells
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[PMID: 18077363] |
| KB | IC50 |
1.82 nM
Compound: K00619a, BIBX-1382
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Inhibition of HGF-mediated thymidine incorporation in human KB cells
Inhibition of HGF-mediated thymidine incorporation in human KB cells
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[PMID: 18077363] |
| KB | IC50 |
3200 nM
Compound: K00619a, BIBX-1382
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Inhibition of FCS-mediated thymidine incorporation in human KB cells
Inhibition of FCS-mediated thymidine incorporation in human KB cells
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[PMID: 18077363] |
| Vero | CC50 |
29.1 μM
Compound: 40; BIBX1382
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Cytotoxicity against african green monkey Vero cells
Cytotoxicity against african green monkey Vero cells
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[PMID: 33539089] |
In Vitro
Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice[2].
With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells[2]
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Dosage:10 mg/kg
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Administration:p.o.; daily; 16 days
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Result:Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment.
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Animal Model:Five- to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells[2]
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Dosage:10 mg/kg (Pharmacokinetic Analysis)
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Administration:p.o.; daily; 16 days
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Result:The C4h is 2222 nM and the C24h is 244 nM.
Chemical Information
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No. CAS 196612-93-8
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Appearance Solid
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Peso molecular 387.84
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Fòrmula C18H19ClFN7
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Color Light yellow to khaki
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SMILES
ClC1=CC(NC2=NC=NC3=CN=C(NC(CC4)CCN4C)N=C23)=CC=C1F
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Synonyms
BIBX 1382
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Neurobiol Dis
ErbB1-dependent signalling and vesicular trafficking in primary afferent nociceptors associated with hypersensitivity in neuropathic pain. [Abstract]2020 Aug:142:104961. PMID: 32531343 -
Front Mol Neurosci
Endocytic Adaptor Protein HIP1R Controls Intracellular Trafficking of Epidermal Growth Factor Receptor in Neuronal Dendritic Development. [Abstract]2018 Dec 6:11:447. PMID: 30574069 -
BMC Cancer
Preclinical studies of the falnidamol as a highly potent and specific active ABCB1 transporter inhibitor. [Abstract]2025 Jan 7;25(1):24. PMID: 39773145 -
Neuroscience
EGFR signaling upregulates surface expression of the GluN2B-containing NMDA receptor and contributes to long-term potentiation in the hippocampus. [Abstract]2015 Sep 24:304:109-21. PMID: 26204818
Falnidamol purchased from MedChemExpress. Usage Cited in: Neuroscience. 2015 Sep 24:304:109-21. [Abstract]
GluN2B Y1472 phosphorylation in whole-cell lysate is increased after 5 and 10 min of EGF treatment in cultured neurons which could be blocked by BIBX-1382. EGFR activation increases SFK activity and phosphorylation of GluN2B Y1472. (A) Representative Western blot result of whole lysate samples from hippocampal slices treated with 50 ng/mL EGF incubation for 10 min. (B) Western blot of EGFR-treated DIV14 cultured hippocampal neurons with minimum glia composition shows increased phosphorylation of
Solvente y solubilidad
In Vitro:
DMSO : 31.25 mg/mL (80.57 mM; ultrasonic and warming and heat to 60°C; 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)
In Vivo:
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: ≥ 1.67 mg/mL (4.31 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Dittrich Ch, et al. Phase I and pharmacokinetic study of BIBX 1382 BS, an epidermal growth factor receptor (EGFR) inhibitor, given in a continuous daily oral administration. Eur J Cancer. 2002 May;38(8):1072-80. [Content Brief]
[2]. Solca FF, et al. Inhibition of epidermal growth factor receptor activity by two pyrimidopyrimidine derivatives. J Pharmacol Exp Ther. 2004 Nov;311(2):502-9. [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 | 2.5784 mL | 12.8919 mL | 25.7838 mL | 64.4596 mL |
| 5 mM | 0.5157 mL | 2.5784 mL | 5.1568 mL | 12.8919 mL | |
| 10 mM | 0.2578 mL | 1.2892 mL | 2.5784 mL | 6.4460 mL | |
| 15 mM | 0.1719 mL | 0.8595 mL | 1.7189 mL | 4.2973 mL | |
| 20 mM | 0.1289 mL | 0.6446 mL | 1.2892 mL | 3.2230 mL | |
| 25 mM | 0.1031 mL | 0.5157 mL | 1.0314 mL | 2.5784 mL | |
| 30 mM | 0.0859 mL | 0.4297 mL | 0.8595 mL | 2.1487 mL | |
| 40 mM | 0.0645 mL | 0.3223 mL | 0.6446 mL | 1.6115 mL | |
| 50 mM | 0.0516 mL | 0.2578 mL | 0.5157 mL | 1.2892 mL | |
| 60 mM | 0.0430 mL | 0.2149 mL | 0.4297 mL | 1.0743 mL | |
| 80 mM | 0.0322 mL | 0.1611 mL | 0.3223 mL | 0.8057 mL |
Falnidamol Related Classifications
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