This product is for research use only, not for human use. We do not sell to patients.
| Size | Price | Stock |
|---|---|---|
| 10mg | $180 | To Be Confirmed |
| 25mg | $315 | To Be Confirmed |
| 50mg | $470 | To Be Confirmed |
| 100mg | $708 | To Be Confirmed |
| 250mg | $1240 | To Be Confirmed |
| 500mg | $1750 | To Be Confirmed |
: Cat #: V3743 CAS #: 1216920-18-1 Purity ≥ 98%
Description: 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.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 460.76 |
|---|---|
| Molecular Formula | C18H21Cl3FN7 |
| CAS No. | 1216920-18-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: ≥ 41 mg/mL |
| Water: | |
| Ethanol: | |
| Solubility In Vivo | CN1CCC(NC2=NC=C(N=CN=C3NC4=CC=C(F)C(Cl)=C4)C3=N2)CC1.[H]Cl.[H]Cl |
| Synonyms | Falnidamol 2HCl; Falnidamol diHCl; BIBX 1382 2HCl;; BIBX1382; BIBX-1382; BIBX 1382BS 2HCl;; BIBX1382BS; BIBX-1382BS |
| Protocol | In Vitro | In vitro activity: 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 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 | |
| Animal model | Nude mice |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1703 mL | 10.8516 mL | 21.7033 mL | 43.4065 mL |
| 5mM | 0.4341 mL | 2.1703 mL | 4.3407 mL | 8.6813 mL |
| 10mM | 0.2170 mL | 1.0852 mL | 2.1703 mL | 4.3407 mL |
| 20mM | 0.1085 mL | 0.5426 mL | 1.0852 mL | 2.1703 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.