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Falnidamol

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

Falnidamol

Purity: 96.46%
Catalog No. TQ0271Alias BIBX 1382Cas No. 196612-93-8
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.
Pack SizePriceAvailabilityQuantity
2 mg$35In Stock
5 mg$58In Stock
10 mg$103In Stock
25 mg$202In Stock
50 mg$353In Stock
100 mg$487In Stock
200 mg$679In Stock
1 mL x 10 mM (in DMSO)$58In Stock
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Purity:96.46%
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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
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].
AliasBIBX 1382
Chemical Properties
Molecular Weight387.84
FormulaC18H19ClFN7
Cas No.196612-93-8
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 28.8 mg/mL (74.3 mM), Sonication and heating to 60℃ are recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5784 mL12.8919 mL25.7838 mL128.9191 mL
5 mM0.5157 mL2.5784 mL5.1568 mL25.7838 mL
10 mM0.2578 mL1.2892 mL2.5784 mL12.8919 mL
20 mM0.1289 mL0.6446 mL1.2892 mL6.4460 mL
50 mM0.0516 mL0.2578 mL0.5157 mL2.5784 mL

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