Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T16996 |
TAS6417
|
Apoptosis; EGFR | Angiogenesis; Apoptosis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
TAS6417 是一种高效的、具有口服活性的 EGFR 突变型抑制剂,可独特的结合到 EGFR 铰链区的 ATP 结合位点,其 IC50值为 1.1-8.0 nM。 | |||
T2490 |
Osimertinib
AZD-9291,Mereletinib,奥希替尼 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Osimertinib (AZD-9291) 是一种 EGFR 三代抑制剂,抑制二代 EGFR 抑制剂产生的 T790M 耐药突变,具有不可逆性和口服活性。Osimertinib 具有抗肿瘤活性,用于治疗 EGFR 突变的非小细胞肺癌。 | |||
T3634 |
Osimertinib mesylate
甲磺酸奥希替尼,Mereletinib mesylate,奥希替尼甲磺酸盐,AZD-9291 mesylate |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Osimertinib mesylate (Mereletinib mesylate) 是一种不可逆的突变选择性 EGFR 抑制剂,对EGFRL858R 和EGFRL858R/T790M 的IC50值分别为 12 和 1 nM。 | |||
T15044 |
D609
|
Apoptosis; Antioxidant | Apoptosis; oxidation-reduction |
D609 (Tricyclodecan-9-yl-Xanthogenate) 具有广泛的生物活性,包括抗氧化、抗凋亡、抗胆碱能、抗肿瘤、抗炎、抗病毒、抗增殖和神经保护活性。D609 通过引起磷脂酰胆碱 (PC) 特异性磷脂酶 C (PC-PLC) 和鞘磷脂合酶 (SMS) 的竞争性抑制来发挥作用。 | |||
T61935 |
B-Raf IN 9
|
||
B-Raf IN 9 (compound 8b) 是有效的B-Raf 抑制剂(IC50= 24.79 nM)。B-Raf IN 9 将细胞周期阻滞于 G2/M 期,诱导凋亡。B-Raf IN 9 对人前列腺癌 PC-3 细胞表现出较强的抗肿瘤活性(IC50= 7.83 μM)。 | |||
T79152 |
PROTAC EGFR degrader 8
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
PROTACEGFRdegrader 8 (T-184) 是一种能够定向降解EGFR的PROTACEGFR降解剂,其在HCC827细胞中的DC50为15.56 nM。该化合物有效抑制多种肺癌细胞系,包括H1975、PC-9和HCC827,其IC50分别为7.72 nM、121.9 nM和14.21 nM。PROTACEGFRdegrader 8 主要用于研究非小细胞肺癌(NSCLC)。 | |||
T37585 | Ensartinib | ||
Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. The ability of Ensartinib (X-396) to inhibit the growth of different cancer cell lines harboring ALK fusions or point mutations is tested. Ensartinib is potent in H3122 lung cancer cells harboring EML4-ALK E13;A20 (IC50: 15nM). Ensartinib is also potent in H2228 lung cancer cells harboring EML4-ALK E6a/b; A20 (IC50: 45 nM). Furthermore, X-376 is potent in SUDHL-1 lymphoma cells harboring N... | |||
T35897 |
ASK120067
|
||
ASK120067 is a potent and orally active inhibitor of EGFRT790M (IC50:0.3 nM) with selectivity over EGFRWT (IC50:6.0 nM). ASK120067 is a third-generation EGFR-TKI for the research of non-small cell lung cancer (NSCLC)[1]. In the in vitro kinase assay ASK120067 potently inhibits the EGFR L858R/T790M and EGFR T790M resistant mutants with IC50 values of 0.3 nM and 0.5 nM, respectively, as well as the EGFRexon19del sensitizing mutant (IC50= 0.5 nM). The 50 of ASK120067 against wild-type EGFR (EGFRWT... |