[CAS NO. 850140-73-7] Afatinib (BIBW2992) Dimaleate

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PRODUCTS SPECIFICATIONS [850140-73-7]

Catalog

SLK-S7810

Brand

Selleck

CAS

850140-73-7

DESCRIPTION [850140-73-7]

Overview

MDL	MFCD25974239
Molecular Weight	717.18
Molecular Formula	C24H25ClFN5O3.2C4H4O4
SMILES	C(=C\C(O)=O)\C(O)=O.N(C=1C2=C(C=C(O[C@H]3CCOC3)C(NC(/C=C/CN(C)C)=O)=C2)N=CN1)C4=CC(Cl)=C(F)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Afatinib (BIBW2992) Dimaleate irreversibly inhibits including , , EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces .

Targets

EGFR (L858R) ^[1] (Cell-free assay)	EGFR (wt) ^[1] (Cell-free assay)	EGFR (L858R/T790M) ^[1] (Cell-free assay)	HER2 ^[1] (Cell-free assay)
0.4 nM	0.5 nM	10 nM	14 nM

In vitro

BIBW2992 is more effective than erlotinib, geﬁtinib, or lapatinib in inhibiting survival of lung cancer cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR. BIBW2992 is similarly effective against NSCLC lines expressing HER2 776insV (NCI-H1781) or EGFR E746_A750del (HCC827), but shows no activity toward A549 cells, which express wild-type EGFR and HER2. Afatinib enhances cytotoxicity of topotecan and mitoxantrone to SP cells, and increases the apoptosis induced by topotecan and mitoxantrone in SP cells.

In vivo

In the MDA-MB-453 xenograft model, BIBW2992 (20 mg/kg, p.o.) results in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%, and downregulation of EGFR and AKT phosphorylation. In A7, A431, FaDu, UT-SCC-14 and UT-SCC-15 xenograft models, application of BIBW 2992 (30 mg/kg, p.o.) leads to a significant prolongation of tumour growth time. In HER2-amplified xenograft medel, Afatinib (30 mg/kg, p.o.) results a markedly inhibition in tumor growth and a significant improvement in the duration of overall survival. In HER2-positive gastric cancer NCI-N87 xenograft, afatinib (25 mg/kg, p.o.) leads to dramatic tumor volume regression within 4 d and near-complete tumor resolution after 21 d of treatment.

References

[1] D Li, et al. Oncogene. 2008, 27(34):4702-4711.
[2] Wang XK, et al. Cancer Res. 2014, 74(16):4431-4445.
[3] Gurtner K, et al. Radiat Oncol. 2014, 9:261.
[4] Schwab CL, et al. Br J Cancer. 2014, 111(9):1750-1756.
[5] Janjiqian YY, et al. J Nucl Med. 2013, 54(6):936-943.

Synonyms

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, (2E)-, (2Z)-2-butenedioate (1:2)

Afatinib dimaleate

BIBW 2992MA2