Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T21312 |
Afatinib
阿法替尼,Afatinib free base,BIBW 2992 |
EGFR; Autophagy | Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Afatinib (BIBW 2992) 是一种不可逆的 EGFR 家族抑制剂,抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。 | |||
T1773 |
Afatinib Dimaleate
马来酸阿法替尼,双马来酸盐阿法替尼,BIBW2992,Afatinib,BIBW 2992MA2,Afatinib (BIBW2992) Dimaleate |
EGFR; HER; Autophagy | Angiogenesis; Autophagy; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Afatinib Dimaleate (BIBW 2992MA2) 是一种可口服的苯胺基-喹唑啉衍生物和受体酪氨酸激酶表皮生长因子受体家族的抑制剂,具有抗肿瘤活性。它抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。 | |||
T2303 |
(S)-Afatinib
BIBW2992,阿法替尼 |
EGFR; HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
(S)-Afatinib (BIBW2992) 是一种不可逆的 EGFR 家族抑制剂,对 EGFRwt、EGFR (L858R)、EGFR (L858R/T790M)、HER2 和 HER4 的 IC50 分别为 0.5/0.4/10/14/1 nM。 | |||
T35430 | Afatinib impurity 11 | ||
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. | |||
T72912 |
(R)-Afatinib
(R)-BIBW 2992 |
||
(R)-Afatinib ((R)-BIBW 2992) 是 Afatinib 异构体。Afatinib 是一种口服有效且不可逆的 ErbB 家族 (EGFR 和HER2) 双特异性抑制剂,对 EGFRwt, EGFRL858R, EGFRL858R/T790M 和 HER2 的 IC50值分别为 0.5 nM、0.4 nM、10 nM 和 14 nM。Afatinib 可用于食管鳞状细胞癌 (ESCC)、非小细胞肺癌 (NSCLC) 和胃癌的研究。 | |||
T10257 | Afatinib N-Oxide | Others | Others |
Afatinib N-Oxide is an impurity of Afatinib in oxidative degradation. Afatinib is an irreversible EGFR family inhibitor. | |||
T10256 |
Afatinib D6
BIBW 2992 D6 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Afatinib D6 (BIBW 2992 D6) is a deuterium-labeled Afatinib. Afatinib is an irreversible EGFR family inhibitor. | |||
T64075 |
Afatinib oxalate
|
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Afatinib (BIBW 2992) oxalate 是一种不可逆的、口服具有活力的 ErbB 家族 (EGFR 和 HER2) 双特异性抑制剂,能够作用于 EGFRwt (IC50: 0.5 nM)、EGFRL858R (IC50: 0.4 nM)、EGFRL858R/T790M (IC50: 10 nM) 和 HER2 (IC50: 14 nM)。Afatinib oxalate 能够用于研究食管鳞状细胞癌 (ESCC)、非小细胞肺癌 (NSCLC) 和胃癌。 | |||
T80574 |
Becotatug
JMT-101 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Becotatug (JMT-101)为一种针对EGFR的IgG1类单克隆抗体,具备与Afatinib及Osimertinib偶联生成ADC(抗体偶联药物)的潜力。 | |||
T69498 | DBPR112 HCl | ||
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 alon... |