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Cat. No.: HY-10261E

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(R)-Afatinib

(Synonyms: (R)-BIBW 2992)

(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?EGFR^wt, EGFR^L858R,?EGFR^L858R/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
Formule: C₂₄H₂₅ClFN₅O₃
Masse moléculaire:485.94

Stockage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

(R)-Afatinib Chemical Structure

CAS No.: 439081-17-1

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

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- Cellular Effect
Chemical Information
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Activité biologique

Description

Voir tous les produits spécifiques à Isoform EGFR :

Voir tous les produits spécifiques à Isoform p38 MAPK :

Cellular Effect

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
Masse moléculaire 485.94
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Li D, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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(R)-Afatinib

Voir tous les produits spécifiques à Isoform EGFR

Voir tous les produits spécifiques à Isoform p38 MAPK

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

(R)-Afatinib Related Classifications

HY-10261E Related Classifications