Cat. No.: HY-10322

Falnidamol

(Synonyms: BIBX 1382)

4 Cited Publications

Customer Review

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.

For research use only. We do not sell to patients.

Purity: 99.41%
CAS No.: 196612-93-8
Formula: C₁₈H₁₉ClFN₇
Molecular Weight:387.84

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Falnidamol Chemical Structure

CAS No.: 196612-93-8

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Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EGFR

3 nM (IC₅₀)

ErbB2

3.4 μM (IC₅₀)

All EGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
KB	IC₅₀	0.15 nM Compound: K00619a, BIBX-1382	Inhibition of EGF-mediated thymidine incorporation in human KB cells Inhibition of EGF-mediated thymidine incorporation in human KB cells	[PMID: 18077363]
KB	IC₅₀	1.82 nM Compound: K00619a, BIBX-1382	Inhibition of HGF-mediated thymidine incorporation in human KB cells Inhibition of HGF-mediated thymidine incorporation in human KB cells	[PMID: 18077363]
KB	IC₅₀	3200 nM Compound: K00619a, BIBX-1382	Inhibition of FCS-mediated thymidine incorporation in human KB cells Inhibition of FCS-mediated thymidine incorporation in human KB cells	[PMID: 18077363]
Vero	CC₅₀	29.1 μM Compound: 40; BIBX1382	Cytotoxicity against african green monkey Vero cells Cytotoxicity against african green monkey Vero cells	[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 (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment^[2].
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 C_4h is 2222 nM and the C_24h is 244 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells^[2]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 16 days
Result:

Completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment.

Animal Model:

Five- to six-week-old athymic NMRI-nu/nu female mice (21–31 g) with A431 cells^[2]
Dosage:

10 mg/kg (Pharmacokinetic Analysis)
Administration:

p.o.; daily; 16 days
Result:

The C_4h is 2222 nM and the C_24h is 244 nM.

Chemical Information

CAS No. 196612-93-8
Appearance Solid
Molecular Weight 387.84
Formula C₁₈H₁₉ClFN₇
Color Light yellow to khaki
SMILES

ClC1=CC(NC2=NC=NC3=CN=C(NC(CC4)CCN4C)N=C23)=CC=C1F
Synonyms

BIBX 1382
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

All WB

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Journal Impact Factor

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 Jul 20;304:109-121. PMID: 26204818

Falnidamol purchased from MedChemExpress. Usage Cited in: Neuroscience. 2015 Jul 20;304:109-121. [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

Solvent & Solubility

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5784 mL

12.8919 mL

25.7838 mL

5 mM

0.5157 mL

2.5784 mL

5.1568 mL

10 mM

0.2578 mL

1.2892 mL

2.5784 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Falnidamol

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Orally Active Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) Falnidamol

All EGFR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Falnidamol Related Classifications

HY-10322 Related Classifications