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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 Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $35 | In Stock | |
5 mg | $58 | In Stock | |
10 mg | $103 | In Stock | |
25 mg | $202 | In Stock | |
50 mg | $353 | In Stock | |
100 mg | $487 | In Stock | |
200 mg | $679 | In Stock | |
1 mL x 10 mM (in DMSO) | $58 | In Stock |
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]. |
Alias | BIBX 1382 |
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 | Powder: -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
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