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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5390 |
BMS-599626 Hydrochloride
AC480 Hydrochloride |
HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
BMS-599626 Hydrochloride (AC480 Hydrochloride) 是一种口服生物有效的HER1、HER2和HER4酪氨酸激酶抑制剂(IC50分别为22、32和190 nM),具有潜在的抗肿瘤活性。BMS-599626 Hydrochloride 抑制人表皮生长因子受体HER1, HER2和HER4,从而抑制过表达这些受体的肿瘤细胞的增殖。 | |||
T11213 |
Epertinib hydrochloride
S-22611 hydrochloride |
EGFR; HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Epertinib hydrochloride (S-22611 hydrochloride) 是口服可逆的选择性EGFR、HER2和HER4抑制剂,IC50值分别为 1.48、7.15 和 2.49 nM,具有抗肿瘤活性。 | |||
T6719 |
Varlitinib
ASLAN001,ARRY-334543 |
HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Varlitinib (ASLAN001) 是有效,可逆的泛 EGFR 小分子抑制剂,对 HER1,HER2 和 HER4 的 IC50 值分别为7,2,4 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。 | |||
T6039 |
TAK-285
TAK285,TAK 285 |
EGFR; MEK; HER; Aurora Kinase | Angiogenesis; Cell Cycle/Checkpoint; Chromatin/Epigenetic; JAK/STAT signaling; MAPK; Tyrosine Kinase/Adaptors |
TAK-285 是一种新型 HER2 和 EGFR(HER1) 双重抑制剂,IC50 分别为 17 和 23 nM。它可穿过血脑屏障,有抗肿瘤活性,对 HER1/2 的选择性是 HER4 的 10 倍以上。 | |||
T5398 |
BMS 599626 2HCl (873837-23-1(HCl))
AC480 dihydrochloride |
HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
BMS 599626 2HCl (873837-23-1(HCl)) (AC480 dihydrochloride) 是 HER1 和 HER2 的选择性抑制剂(IC50:20 nM 和 30 nM),对 HER4 的效力降低约 8 倍,对 Lck、VEGFR2、c-Kit、MET 等的效力降低 100 倍以上。 | |||
T8758 |
Poziotinib hydrochloride
HM 781-36B hydrochloride,NOV120101 hydrochloride,波齐替尼盐酸盐 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Poziotinib hydrochloride 不可逆地抑制 EGFR(HER1 或 ErbB1),包括 EGFR 突变体、HER2 和 HER4,从而抑制过度表达这些受体的肿瘤细胞的增殖。它是一种口服生物可利用的、基于喹唑啉的泛表皮生长因子受体(EGFR 或 HER)抑制剂,具有潜在的抗肿瘤活性。 | |||
T5168 |
EGFR-IN-12
EGFR Inhibitor |
Apoptosis; EGFR | Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
EGFR-IN-12 (EGFR Inhibitor) 是一种 4,6-二取代的嘧啶,可诱导细胞凋亡,具有抗肿瘤活性。它是ATP 竞争性,不可逆且高度选择性的EGFR 抑制剂,IC50为 21 nM。它对EGFR 的选择性高于 HER4 和 55种其他激酶。它还抑制突变型EGFRL858R 和EGFRL861Q,IC50分别为 63 nM 和 4 nM。 | |||
T11213L |
Epertinib
S-22611 |
EGFR; HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor activity. | |||
T2610L |
BMS-599626 2HCL(714971-09-2 Free base)
BMS 599626 dihydrochloride,BMS-599626 2HCL(714971-09-2 Free base),AC480 2HCl |
HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
BMS-599626 2HCL (AC480 2HCl) 是BMS-599626 衍生物。BMS-599626 是一种可口服且具有选择性的 HER1 和 HER2 双重抑制剂, IC50 分别为 20 和 30 nM。BMS-599626 抑制肿瘤细胞增殖,并有可能增加肿瘤对放疗的反应。 | |||
T2630 |
Poziotinib
HM781-36B,NOV120101 |
Apoptosis; EGFR; HER | Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Poziotinib (NOV120101) 是一种不可逆的 HER1/2/4 抑制剂 (IC50s: 3/5/23 nM)。 | |||
T34760 |
SYR127063
SYR-127063,BDBM 92454,SYR 127063,BDBM-92454,BDBM92454 |
EGFR; HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
SYR127063 (BDBM-92454) 是一种有效的选择性 HER2 抑制剂,以反应构象与 HER2 结合。 | |||
T62047 |
pan-HER-IN-1
|
Others | Others |
pan-HER-IN-1 (Compound C5) 是不可逆的、口服有效的广谱HER 抑制剂。pan-HER-IN-1抑制EGFR、HER4、EGFRT790M/L858R 和HER2的活性,IC50分别为 0.38、1.6、2.2 和 3.5 nM。pan-HER-IN-1可以诱导细胞凋亡 (apoptosis),显示出抗肿瘤活性。 | |||
T62621 |
pan-HER-IN-2
|
Others | Others |
pan-HER-IN-2 (Compound C6) 是一种口服具有活力的、可逆的广谱 HER 抑制剂,能够作用于 EGFR (IC50: 0.72 nM)、HER4 (IC50: 2.0 nM)、EGFRT790M (IC50: 8.2 nM) / L858R (IC50: 75.1 nM)。pan-HER-IN-2 可以诱导细胞凋亡 (apoptosis),具有抗肿瘤作用。 | |||
T14677 |
BMS-690514
|
EGFR; VEGFR; HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
BMS-690514是可口服的EGFR 和VEGFR 抑制剂,对于EGFR、HER2和HER4的IC50值分别为5、9 和 60 nM。 | |||
T2610 |
BMS-599626
AC480 |
EGFR; MEK; HER; Src | Angiogenesis; JAK/STAT signaling; MAPK; Tyrosine Kinase/Adaptors |
BMS-599626 (AC480) 是可口服的选择性 HER1和HER2抑制剂,IC50分别为 20 和 30 nM。它对 HER4 的 IC50值为 190 nM,可抑制肿瘤细胞增殖,有治疗肿瘤的潜力。 | |||
T7819 |
TAS0728
|
EGFR; HER | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
TAS0728 是一种 HER2 抑制剂,与HER2的 C805 位点共价结合,IC50值为 13 nM。它抑制 HER2、HER3 及其下游效应蛋白的磷酸化,具有抗肿瘤活性。 |
Cat. No. | Product Name | Species | Expression System |
---|---|---|---|
TMPK-00448 |
HER4/ERBB4 Protein, Human, Recombinant (His & Avi)
HER4,ALS19,4ICD,p180erbB4 |
Human | HEK293 Cells |
Her4, a member of the EGF receptor family, plays a variety of roles in physiological and pathological states. Genetic studies have indicated a link between Her4 and type 2 diabetes and obesity. Her4 may play an important role in glucose homeostasis and lipogenesis. Her4 deficiency-related obesity and adipose tissue inflammation may contribute to the development of MetS. HER4/ERBB4 Protein, Human, Recombinant (His & Avi) is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted mol... | |||
TMPK-00449 |
HER4/ERBB4 Protein, Human, Recombinant (His & Avi), Biotinylated
E4ICD,ALS19,ErbB4,4ICD,HER |
Human | HEK293 Cells |
Her4, a member of the EGF receptor family, plays a variety of roles in physiological and pathological states. Genetic studies have indicated a link between Her4 and type 2 diabetes and obesity. Her4 may play an important role in glucose homeostasis and lipogenesis. Her4 deficiency-related obesity and adipose tissue inflammation may contribute to the development of MetS. HER4/ERBB4 Protein, Human, Recombinant (His & Avi), Biotinylated is expressed in HEK293 mammalian cells with C-His-Avi tag. The... | |||
TMPY-03021 |
ErbB4 Protein, Mouse, Recombinant (His)
c-erbB-4,Her4,erb-b2 receptor tyr... |
Mouse | HEK293 Cells |
ErbB4 Protein, Mouse, Recombinant (His) is expressed in HEK293 mammalian cells with His tag. The predicted molecular weight is 71.5 kDa and the accession number is Q99P91. | |||
TMPY-02246 |
HB-EGF Protein, Human, Recombinant
DTSF,DTR,HEGFL,heparin-binding EGF-like growth factor,DTS |
Human | Baculovirus Insect Cells |
Heparin-binding EGF-like growth factor (HBEGF), a member of the EGF family of growth factors, exerts its biological activity through activation of the EGFR and other ErbB receptors. Soluble mature HBEGF is proteolytically processed from a larger membrane-anchored precursor and is a potent mitogen and chemotactic factor for fibroblasts, smooth muscle cells but not endothelial cells. HBEGF activates two EGF receptor subtypes, HER1 and HER4, and binds to cell surface HSPG. The transmembrane form of... |