(R)-Afatinib
(R)-Afatinib ((R)-BIBW 2992) is the Afatinib isomer. Afatinib (HY-10261) is an orally active, potent and irreversible dual specificity inhibitor of?ErbB?family (EGFR?and?HER2), with?IC50?values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for?EGFRwt, EGFRL858R,?EGFRL858R/T790M?and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung?cancer?(NSCLC) and gastric?cancer.
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- CAS No.: 439081-17-1
- 화학식: C24H25ClFN5O3
- 분자량:485.94
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
<0.001 μM
Compound: BIBW2992
|
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
|
[PMID: 28987609] |
| A549 | IC50 |
0.71 μM
Compound: 3
|
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
|
[PMID: 29775935] |
| BT-474 | IC50 |
54 nM
Compound: 34; BIBW2992
|
Antiproliferative activity against human BT474 cells expressing wild type HER2 incubated for 72 hrs by MTS assay
Antiproliferative activity against human BT474 cells expressing wild type HER2 incubated for 72 hrs by MTS assay
|
[PMID: 28754471] |
| MCF7 | IC50 |
0.93 μM
Compound: 3
|
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
|
[PMID: 29775935] |
| NCI-H1975 | IC50 |
0.495 μM
Compound: BIBW2992
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
|
[PMID: 28987609] |
| NCI-H1975 | IC50 |
92 nM
Compound: 34; BIBW2992
|
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant incubated for 72 hrs by MTS assay
|
[PMID: 28754471] |
| PC-3 | IC50 |
2.51 μM
Compound: 3
|
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
|
[PMID: 29775935] |
Chemical Information
-
CAS No. 439081-17-1
-
분자량 485.94
-
화학식 C24H25ClFN5O3
-
SMILES
CN(C)C/C=C/C(NC1=CC(C(NC2=CC(Cl)=C(C=C2)F)=NC=N3)=C3C=C1O[C@@H]4CCOC4)=O
-
Synonyms
(R)-BIBW 2992
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)