Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T16162 |
Mutated EGFR-IN-1
Osimertinib analog,AZD9291中间体1 |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Mutated EGFR-IN-1 (Osimertinib analog) 是用于突变 EGFR 抑制剂设计的有用中间体,例如 L858R EGFR、Exon19 缺失激活突变体和 T790M 抗性突变体。 | |||
T10433 |
Osimertinib dimesylate
奥希替尼二甲磺酸盐,Mereletinib (dimesylate),AZD-9291 (dimesylate) |
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M). | |||
T72818 |
Dosimertinib-d
|
||
Dosimertinib-d3是一种有效的口服活性EGFR 抑制剂。Dosimertinib-d3降低 p-EGFR 和 p-ERK 蛋白水平的表达。Dosimertinib-d3显示出抗增殖和抗肿瘤活性。Dosimertinib-d3具有非小细胞肺癌 (NSCLC) 研究的潜力。 | |||
T8327 |
ONO-7475
|
Trk receptor; TAM Receptor | Tyrosine Kinase/Adaptors |
ONO-7475 是一种选择性的、有效的、具有口服活性的Axl/Mer 抑制剂。它使 AXL 过表达的EGFR 突变型 NSCLC 细胞对 EGFR-TKIs 敏感,抑制耐药细胞的产生和耐药性的维持。它与 Osimertinib 联合使用,具有用于 EGFR 突变非小细胞肺癌的潜力。 | |||
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。 | |||
T82193 |
HJM-561
|
PROTACs | PROTAC |
HJM-561为一种有效的选择性口服生物可利用EGFRPROTAC,能够克服osimertinib耐药的EGFR三重突变,并表现出抗肿瘤活性。 | |||
T74641 | Rezivertinib analogue 1 | ||
Rezivertinib analogue 1 是一种甲磺酸奥希替尼的工艺杂质, 可用于非小细胞肺癌的研究。 | |||
T74982 |
Akt3 degrader 1
|
||
Akt3degrader 1 (化合物 12l) 是一种选择性的Akt3降解剂,能克服Osimertinib 诱导的 H1975OR NSCLC 细胞的抗性。Akt3degrader 1 还具有抗增殖活性,能显著抑制小鼠体内肿瘤的生长。Akt3degrader 1 可用于耐药性非小细胞肺癌的研究。 | |||
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... | |||
T70128 |
Olmutinib hydrochloride
|
||
Olmutinib is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor, used in the treatment of T790M mutation positive non-small cell lung cancer. Olmutinib covalently binds a cysteine residue near the kinase domain of mutant EGFRs to prevent phosphorylation of the receptor. EGFRs are frequently over-expressed in lung cancer and contribute to activation of the phosphoinositide 3-kinase and mitogen-activated protein kinase pathways which both p... | |||
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... |