|
Product Name: |
Afatinib(BIBW 2992) |
|
Synonyms: |
Tovok;BIBW 2992;N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2-butenamide;Afatinb;(S)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dim;Afatinib(cis-trans isomerismtautomers);Afatinib(W.S);AFATINIB; BIBW2992;BIBW-2292 |
|
CAS: |
439081-18-2 |
|
MF: |
C24H25ClFN5O3 |
|
MW: |
485.94 |
|
EINECS: |
1308068-626-2 |
Afatinib(BIBW 2992) Physical and Chemical Properties
| Melting point | 100-102℃ |
| Boiling point | 676.9±55.0 °C(Predicted) |
| density | 1.380 |
| storage temp. | Store at -20°C |
| solubility | ≥24.3 mg/mL in DMSO; insoluble in H2O; ≥42.1 mg/mL in EtOH with ultrasonic |
| form | solid |
| pka | 12.06±0.43(Predicted) |
Afatinib(BIBW 2992) Usage And Synthesis
|
Uses |
BIBW2992 (Afatinib, Tomtovok, Tovok) irreversibly inhibits EGFR/HER2 including EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively. |
Mechanism of action
Afatinib is the first approved irreversible ErbB series blocker. The ErbB receptor family consists of 4 members: EGFR (ErbB1), HER2 (ErbB2), ErbB3 and ErbB4. ErbB family members communicate with other ErbB family members. Abnormal ErbB family signal transduction is a key driving factor for the growth and spread of cancer cells. Afatinib has two targets of EGFR and HER2, which can irreversibly block the internal stimulation of cells due to the mutation of epidermal growth factor receptor (EGFR) and the overexpression of human epidermal receptor 2 (HER2) tyrosine kinase Abnormal information conduction permanently closes the signal transduction channel on which cancer cells depend for survival, preventing cancer cells from growing and reproducing, thereby curing cancer.
Hot Tags: afatinib cas no.439081-18-2, China, manufacturers, suppliers, factory, custom, wholesale, Atazanavir Intermediates, CAS NO 191732 72 6, Lenalidomide
