BIBU-1361 is an EGFR inhibitor. BIBU1361 blocked epidermal growth factor-induced phosphorylation of EGFR and also prevented downstream responses such as mitogen-activated protein kinase kinase (MAPK/extracellular signal-regulated kinase kinase) and MAPK activation in cells. In accordance with these observations thymidine incorporation into EGFR-expressing KB cells was selectively and potently inhibited by BIBU1361 with half-maximally effective doses in the nanomolar range. Oral administration of BIBU-1361 inhibited the growth of established human xenografts in athymic mice, including vulval and head and neck squamous cell carcinomas.
MedKoo Cat#: 574587
Name: BIBU-1361 HCl
CAS#: 1643609-75-9 (HCl)
Chemical Formula: C22H29Cl3FN7
Exact Mass: 515.1534
Molecular Weight: 516.87
Elemental Analysis: C, 51.12; H, 5.66; Cl, 20.58; F, 3.68; N, 18.97
| Solvent | mg/mL | mM | comments | |
|---|---|---|---|---|
| Solubility | ||||
| DMSO | 12.9 | 25.00 | ||
| Water | 51.7 | 100.00 |
The following data is based on the product molecular weight 516.87 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
