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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...

化合物

Osimertinib
Cat.No: T2490
Synonym: AZD-9291,Mereletinib,奥希替尼
Target: EGFR
Osimertinib mesylate
Cat.No: T3634
Synonym: 甲磺酸奥希替尼,Mereletinib mesylate,奥希替尼甲磺酸盐,AZD-9291 mesylate
Target: EGFR
Mutated EGFR-IN-1
Cat.No: T16162
Synonym: Osimertinib analog,AZD9291中间体1
Target: EGFR
Osimertinib dimesylate
Cat.No: T10433
Synonym: 奥希替尼二甲磺酸盐,Mereletinib (dimesylate),AZD-9291 (dimesylate)
Target: EGFR
Dosimertinib-d
Cat.No: T72818
Synonym:
Target:
ONO-7475
Cat.No: T8327
Synonym:
Target: Trk receptor, TAM Receptor
Becotatug
Cat.No: T80574
Synonym: JMT-101
Target: EGFR
HJM-561
Cat.No: T82193
Synonym:
Target: PROTACs
Rezivertinib analogue 1
Cat.No: T74641
Synonym:
Target:
Akt3 degrader 1
Cat.No: T74982
Synonym:
Target:
DBPR112 HCl
Cat.No: T69498
Synonym:
Target:
Olmutinib hydrochloride
Cat.No: T70128
Synonym:
Target:
ASK120067
Cat.No: T35897
Synonym:
Target:
TargetMol Loading
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