CAS 439081-18-2|Afatinib (BIBW2992)

Introduction：Basic information about CAS 439081-18-2|Afatinib (BIBW2992), including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Afatinib (BIBW2992) BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Customs
6. Synonyms

Common Name	Afatinib (BIBW2992)
CAS Number	439081-18-2	Molecular Weight	485.94
Density	1.4±0.1 g/cm3	Boiling Point	676.9±55.0 °C at 760 mmHg
Molecular Formula	C₂₄H₂₅ClFN₅O₃	Melting Point	100 - 102 °C
MSDS	/	Flash Point	363.2±31.5 °C

Names

Name	Afatinib
Synonym	More Synonyms

Afatinib (BIBW2992) BiologicalActivity

Description	(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells[1].
Related Catalog	Signaling Pathways >>Apoptosis >>ApoptosisSignaling Pathways >>JAK/STAT Signaling >>EGFRResearch Areas >>OthersSignaling Pathways >>Protein Tyrosine Kinase/RTK >>EGFRSignaling Pathways >>Autophagy >>AutophagySignaling Pathways >>MAPK/ERK Pathway >>p38 MAPKSignaling Pathways >>PI3K/Akt/mTOR >>AktSignaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFR
References	[1]. Yoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109(4):1166-1176. [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. [3]. 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. [4]. 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.

Description

(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells[1].

Related Catalog

Signaling Pathways >>Apoptosis >>ApoptosisSignaling Pathways >>JAK/STAT Signaling >>EGFRResearch Areas >>OthersSignaling Pathways >>Protein Tyrosine Kinase/RTK >>EGFRSignaling Pathways >>Autophagy >>AutophagySignaling Pathways >>MAPK/ERK Pathway >>p38 MAPKSignaling Pathways >>PI3K/Akt/mTOR >>AktSignaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFR

References

[1]. Yoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109(4):1166-1176.

[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.

[3]. 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.

[4]. 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.

Chemical & Physical Properties

Density	1.4±0.1 g/cm3
Boiling Point	676.9±55.0 °C at 760 mmHg
Melting Point	100 - 102 °C
Molecular Formula	C₂₄H₂₅ClFN₅O₃
Molecular Weight	485.94
Flash Point	363.2±31.5 °C
Exact Mass	485.162994
PSA	88.61000
LogP	3.59
Vapour Pressure	0.0±2.1 mmHg at 25°C
Index of Refraction	1.668
Storage condition	-20°C

Safety Information

Hazard Codes	Xn
HS Code	2934999090

Customs

HS Code	2934999090
Summary	2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Synonyms

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, (2E)-

(S,E)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-((tetrahydrofuran-3-yl)oxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide

(2E)-N-(4-[(3-chloro-4-fluorophenyl)amino]-7-{[(3S)-tetrahydrofuran-3-yl]oxy}quinazolin-6-yl)-4-(dimethylamino)but-2-enamide

Afatinib

Tovok

Tomtovok

BIBW2992

(2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-[(3S)-tetrahydro-3-furanyloxy]-6-quinazolinyl}-4-(dimethylamino)-2-butenamide

Gilotrif

BIBW 2992

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