afatinib

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).

Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.

(S)-Afatinib (BIBW2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, respectively.

(R)-Afatinib ((R)-BIBW 2992), an isomer of Afatinib, is a potent, orally administered, irreversible inhibitor targeting the ErbB family (EGFR and HER2) with IC50 values of 0.5 nM for EGFR wt, 0.4 nM for EGFR L858R, 10 nM for EGFR L858R/T790M, and 14 nM for HER2. It holds potential for research into esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer [1].

Afatinib N-Oxide is an impurity of Afatinib in oxidative degradation. Afatinib is an irreversible EGFR family inhibitor.

Afatinib D6 (BIBW 2992 D6) is a deuterium-labeled Afatinib. Afatinib is an irreversible EGFR family inhibitor.

Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1]. [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.

Afatinib (BIBW 2992) oxalate is an irreversible, orally active bispecific inhibitor of the ErbB family (EGFR and HER2) that acts on EGFRwt (IC50: 0.5 nM), EGFRL858R (IC50: 0.4 nM), EGFRL858R/T790M ( IC50: 10 nM) and HER2 (IC50: 14 nM). Afatinib oxalate can be used to study esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

DBPR112 is a potent EGFR inhibitor (IC50=487 nM) as a Clinical Candidate for the Treatment of Non-Small Cell Lung Cancer. DBPR112), DBPR112 not only displayed a potent inhibitory activity against EGFRL858R/T790M double mutations but also exhibited tenfold potency better than the third-generation inhibitor, osimertinib,against EGFR and HER2 exon 20 insertion mutations. Overall, pharmacokinetic improvement through lead-to-candidate optimization yielded fourfold oral AUC better that afatinib along with F = 41.5%, an encouraging safety profile, and significant antitumor efficacy in in vivo xenograft models.

Becotatug (JMT-101) is an IgG1 antibody that targets EGFR and can be conjugated to Afatinib and Osimertinib, functioning as a synthetic antibody-drug conjugate (ADC) [1].