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Falnidamol

Name: Falnidamol
Brand: TargetMol
SKU: TQ0271
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0271Cas No. 196612-93-8

Alias BIBX 1382

Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. It displays >1000-fold lower potency against ErbB2 (IC50=3.4 μM) and other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and exhibits anti-cancer activity.

Falnidamol

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Purity: 98.81%

Catalog No. TQ0271Alias BIBX 1382Cas No. 196612-93-8

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$35	In Stock	In Stock
5 mg	$58	In Stock	In Stock
10 mg	$103	In Stock	In Stock
25 mg	$202	In Stock	In Stock
50 mg	$353	In Stock	In Stock
100 mg	$487	-	In Stock
200 mg	$679	-	In Stock
1 mL x 10 mM (in DMSO)	$58	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:98.81%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. It displays >1000-fold lower potency against ErbB2 (IC50=3.4 μM) and other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and exhibits anti-cancer activity.
Targets&IC50	ErbB2:3.4 μM, EGFR:3 nM
In vitro	Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50: 3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM) [1]. Falnidamol demonstrates antiproliferative activity in mitogenic assays performed with KB cells [2].
In vivo	Falnidamol (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. Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice. With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C4h is 2222 nM and the C24h is 244 nM [2].
Animal Research	Animal Model: Five- to six-week-old athymic NMRI-nu/nu female mice (21-31 g) with A431, FaDu, or HN5 cells 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 [2].
Synonyms	BIBX 1382

Chemical Properties

Molecular Weight	387.84
Formula	C₁₈H₁₉ClFN₇
Cas No.	196612-93-8
Smiles	CN1CCC(CC1)Nc1ncc2ncnc(Nc3ccc(F)c(Cl)c3)c2n1
Relative Density.	1.427 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 28.8 mg/mL (74.26 mM), Sonication and heating to 60℃ are recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (2.58 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5784 mL	12.8919 mL	25.7838 mL	128.9191 mL
5 mM	0.5157 mL	2.5784 mL	5.1568 mL	25.7838 mL
10 mM	0.2578 mL	1.2892 mL	2.5784 mL	12.8919 mL
20 mM	0.1289 mL	0.6446 mL	1.2892 mL	6.4460 mL
50 mM	0.0516 mL	0.2578 mL	0.5157 mL	2.5784 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc