| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
BIBX 1382 targets the epidermal growth factor receptor (EGFR) tyrosine kinase. EGFR is a receptor tyrosine kinase involved in the regulation of cell growth, differentiation, and survival. By inhibiting EGFR kinase activity, BIBX 1382 blocks downstream signaling pathways that promote cell proliferation and survival. The compound has an IC50 of 3 nM for EGFR and shows high selectivity over ErbB2 and other related tyrosine kinases.
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| ln Vitro |
Falnidamol (formerly known as BIBX 1382) is a potent and selective inhibitor EGFR inhibitor with IC50 of 3 nM and potential anticancer activities; it displays > 1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). BIBX1382 and BIBU1361 are both potent and selective submicromolar inhibitors of the EGFR kinase activity. An IC50 value of 3 nM was determined for both compounds. The potency of these two compounds compares with the one obtained with Iressa, which is a leading EGFR inhibitor in the field. Inhibition of the closest family member, HER2, was 100- to 1000-fold less potent. Furthermore, BIBX1382 and BIBU1361 did not inhibit a number of other related tyrosine kinases.
Kinase Assay: BIBX1382 and BIBU1361 are both potent and selective submicromolar inhibitors of the EGFR kinase activity. An IC50 value of 3 nM was determined for both compounds. The potency of these two compounds compares with the one obtained with Iressa, which is a leading EGFR inhibitor in the field. Inhibition of the closest family member, HER2, was 100- to 1000-fold less potent. Furthermore, BIBX1382 and BIBU1361 did not inhibit a number of other related tyrosine kinases. Cell Assay: In vitro, BIBX 1382 is a potent and selective EGFR inhibitor with an IC50 of 3 nM. It displays >1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). The potency of BIBX 1382 compares with that of Iressa (gefitinib), a leading EGFR inhibitor in the field. Inhibition of HER2 was 100- to 1000-fold less potent. |
| ln Vivo |
In nude mice, oral once daily dosing at 10 mg/kg with either BIBX1382 or BIBU1361 completely suppressed tumor growth of human A431 xenografts with respective T/C values of 15 and 6% after 2 weeks of treatment
In nude mice, oral once daily dosing at 10 mg/kg with BIBX 1382 completely suppressed tumor growth of human A431 xenografts with a T/C value of 15% after 2 weeks of treatment. This demonstrates significant in vivo antitumor activity. The compound's oral bioavailability supports its use in animal efficacy studies. Specific details of dosing regimens and efficacy data are described in the referenced studies. |
| Enzyme Assay |
The EGFR kinase inhibition assay for BIBX 1382 involves incubating the compound with recombinant EGFR kinase, ATP, and a peptide substrate. The reaction is carried out in a kinase buffer optimized for EGFR activity. After incubation, the amount of phosphorylated substrate is quantified using a luminescence-based kinase assay (such as ADP-Glo) or a radiometric assay. IC50 values are calculated from dose-response curves. Kinase selectivity is assessed by testing against a panel of related tyrosine kinases.
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| Cell Assay |
To evaluate the cellular activity of BIBX 1382, EGFR-overexpressing cancer cell lines (such as A431 human epidermoid carcinoma cells) are seeded in 96-well plates and treated with varying concentrations of the compound. After 72 hours of incubation, cell proliferation is measured using an MTT or SRB assay. The compound's effect on EGFR phosphorylation and downstream signaling is assessed by Western blot analysis. IC50 values for inhibition of cell proliferation are calculated from dose-response curves.
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| Animal Protocol |
10 mg/kg; oral
Nude mice The in vivo efficacy of BIBX 1382 is evaluated in nude mouse xenograft models using human A431 tumor cells. Tumor cells are implanted subcutaneously into immunodeficient mice. When tumors reach a certain size, mice are randomized into treatment groups and administered BIBX 1382 orally once daily at a dose of 10 mg/kg. Tumor volume and body weight are measured twice weekly. At the end of the treatment period (2 weeks), tumor growth inhibition is calculated as T/C values. |
| ADME/Pharmacokinetics |
BIBX 1382 is characterized as being orally bioavailable, supporting once-daily oral dosing in animal models. Specific pharmacokinetic parameters (e.g., Cmax, Tmax, half-life, AUC) are not detailed in the available sources. The compound has a molecular weight of 532.38 (as diHCl salt) and a molecular formula of C23H24Cl2FN5O2. It is typically stored as a powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BIBX 1382 are not provided in the available sources. In the nude mouse xenograft study, the compound was administered at 10 mg/kg orally once daily without mention of overt toxicity. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. Standard safety precautions should be followed when handling this compound.
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| References |
:J Pharmacol Exp Ther.2004 Nov;311(2):502-9. Epub 2004 Jun 15.
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| Additional Infomation |
BIBX 1382 diHCl is also known as Falnidamol. It is a potent and selective EGFR inhibitor with an IC50 of 3 nM and displays >1000-fold lower potency against ErbB2 (IC50 = 3.4 μM) and a range of other related tyrosine kinases (IC50 > 10 μM). It is supplied for research purposes with a purity of ≥98% and is typically stored at -20°C.
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| Molecular Formula |
C18H21CL3FN7
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| Molecular Weight |
460.76
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| Exact Mass |
459.09
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| CAS # |
1216920-18-1
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| Related CAS # |
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| PubChem CID |
46861540
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
479
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C=CC(=C1)NC1C2=C(C=NC(=N2)NC2CCN(C)CC2)N=CN=1)F.Cl.Cl
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| InChi Key |
RFXGEKWBTCMDAW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H19ClFN7.2ClH/c1-27-6-4-11(5-7-27)25-18-21-9-15-16(26-18)17(23-10-22-15)24-12-2-3-14(20)13(19)8-12;;/h2-3,8-11H,4-7H2,1H3,(H,21,25,26)(H,22,23,24);2*1H
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| Chemical Name |
4-N-(3-chloro-4-fluorophenyl)-6-N-(1-methylpiperidin-4-yl)pyrimido[5,4-d]pyrimidine-4,6-diamine;dihydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1703 mL | 10.8516 mL | 21.7033 mL | |
| 5 mM | 0.4341 mL | 2.1703 mL | 4.3407 mL | |
| 10 mM | 0.2170 mL | 1.0852 mL | 2.1703 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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