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Afatinib

Catalog No. T21312 CAS 850140-72-6

Synonyms: Afatinib free base, BIBW 2992

Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).

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Afatinib, CAS 850140-72-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 30.00
10 mg	In stock	$ 47.00
25 mg	In stock	$ 78.00
50 mg	In stock	$ 117.00
100 mg	In stock	$ 147.00
200 mg	In stock	$ 187.00
500 mg	In stock	$ 316.00
1 mL * 10 mM (in DMSO)	In stock	$ 48.00

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Purity: 99.9%

Purity: 97.56%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).
Targets&IC50	EGFR:0.5 nM, EGFR (L858R/T790M):10 nM, EGFR (L858R):0.4 nM, HER2:14 nM
In vitro	ESCC cell lines were sensitive to afatinib with IC50 concentrations at lower micro-molar range (at 72 hour incubation: HKESC-1 = 0.002 μM, HKESC-2 = 0.002 μM, KYSE510 = 1.090 μM, SLMT-1 = 1.161 μM and EC-1 = 0.109 μM) with a maximum growth inhibition over 95%.?Afatinib can strongly induce G0/G1 cell cycle arrest in HKESC-2 and EC-1 in a dose- and time-dependent manner.?The phosphorylation of ErbB family downstream effectors such as pAKT, pS6 and pMAPK were significantly inhibited in HKESC-2 and EC-1.?Apoptosis was observed in both cell lines at 24 hours after exposure to afatinib, as determined by the presence of cleaved PARP[1].
In vivo	Afatinib could effectively inhibit HKESC-2 tumor growth in mice without obvious toxicity[1].

Synonyms	Afatinib free base, BIBW 2992
Molecular Weight	485.94
Formula	C24H25ClFN5O3
CAS No.	850140-72-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (195.4 mM)

References and Literature

1. Wong CH, et al. Preclinical evaluation of afatinib (BIBW2992) in esophageal squamous cell carcinoma (ESCC). Am J Cancer Res. 2015 Nov 15;5(12):3588-99. 2. Wang XK, et al. Afatinib circumvents multidrug resistance via dually inhibiting ATP binding cassette subfamily G member 2 in vitro and in vivo. Oncotarget. 2014 Dec 15;5(23):11971-85.

Citations

1. Liang J, Bi G, Sui Q, et al.Transcription factor ZNF263 enhances EGFR-targeted therapeutic response and reduces residual disease in lung adenocarcinoma.Cell Reports.2024, 43(2).

Related compound libraries

This product is contained In the following compound libraries：

FDA-Approved Kinase Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library EMA Approved Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Inhibitor Library

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H-9 dihydrochloride Olmutinib EGFR-IN-1 hydrochloride Biochanin A EBE-A22 Patritumab Tesevatinib Marinobufogenin

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Afatinib 850140-72-6 Angiogenesis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR NIH-3T3 cells ESCC NSCLC NCI-H1975 inhibit ErbB-1 HKESC-2 EC-1 PKB H1666 c-Met/HGFR Afatinib free base Apoptosis SLMT-1 H3255 BIBW 2992 A431 BIBW-2992 lung cancer Akt Inhibitor BIBW2992 HER2 Epidermal growth factor receptor HKESC-1 anticancer Protein kinase B orally active p38 MAPK HER1 inhibitor

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