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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.

For research use only. We do not sell to patients.

CAS No.: 439081-17-1
Formula: C₂₄H₂₅ClFN₅O₃
Molecular Weight:485.94

Storage:

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)

Biological Activity
- Description
- Cellular Effect
Chemical Information
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Classifications
Bioz

Biological Activity

Description

All EGFR Isoforms :

All p38 MAPK Isoforms :

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
Molecular Weight 485.94
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Handling Instructions (2659 KB)

References

[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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100 mg

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Biological Activity
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(R)-Afatinib

All EGFR Isoforms

All p38 MAPK Isoforms