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抑制剂 & 化合物

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2032	WHI-P180 Janex 3	EGFR; VEGFR; c-RET; CDK	Angiogenesis; Apoptosis; Cell Cycle/Checkpoint; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	WHI-P180 (Janex 3) 是 EGFR 和 Cdk2 抑制剂，IC50 分别为 4.0 和 1.0 μM。
T1985	WHI-P154 Jak3 inhibitor ii	Apoptosis; EGFR; VEGFR; JAK; Src	Angiogenesis; Apoptosis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells; Tyrosine Kinase/Adaptors
	WHI-P154 (Jak3 inhibitor ii) 是一种 EGFR 抑制剂，也抑制 JAK3的活性，IC50值分别为 4 nM 和 1.8 μM。
T35528	TD52	Apoptosis; Phosphatase; Akt	Apoptosis; Cytoskeletal Signaling; Metabolism; PI3K/Akt/mTOR signaling
	TD52 是 PP2A (CIP2A) 癌性抑制剂的口服活性抑制剂。 TD52 是厄洛替尼衍生物，通过干扰 Elk1 与 CIP2A 启动子的结合间接降低了 CIP2A。
T8431	JCN037	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	JCN037 是能透过血脑屏障的EGFR 共价抑制剂，对 EGFR、p-wtEGFR 和 pEGFRvⅢ 的IC50值分别为 2.49、3.95 和4.48 nM。
T35528L	TD52 dihydrochloride TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl	Others	Others
	TD52 dihydrochloride (TD52 2HCl), a derivative of Erlotinib, is a potent and orally active inhibitor of protein phosphatase 2A (CIP2A). It exhibits strong anti-cancer properties by regulating the CIP2A/PP2A/p-Akt signaling pathway, resulting in the induction of apoptosis in triple-negative breast cancer (TNBC) cells. Mechanistically, TD52 dihydrochloride disrupts the binding of Elk1 to the CIP2A promoter, effectively reducing CIP2A levels. Notably, TD52 dihydrochloride demonstrates powerful anti...
T11157L	EGFR-IN-1 hydrochloride	EGFR	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	EGFR-IN-1 hydrochloride 是 L858R/T790M 突变体 EGFR 的不可逆特异性抑制剂，选择性是野生型 EGFR 的 100 倍。 EGFR-IN-1 hydrochloride 在 H1975 细胞和突变体 HCC827 细胞中表现出有效的抗肿瘤和抗增殖活性，IC50 分别为 4 和 28 nM。
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。
T74833	EGFR T790M/L858R-IN-2
	EGFRT790M/L858R-IN-2是一种有效选择性的EGFRT790M/L858R抑制剂，其对EGFRT790M/L858R和EGFRWT的IC50值分别为3.5nM和1290nM。该化合物能够降低p-EGFR、P-AKT、P-ERK1/2的表达，诱导细胞凋亡及细胞周期在G1期的停滞，显示出抗癌活性。
T72788	EGFR/C797S-IN-1
	EGFR/C797S-IN-1 是一种有效的EGFR-C797S 抑制剂，IC50值为 0.128 µM。EGFR/C797S-IN-1 显示出抗增殖活性和抗肿瘤活性。EGFR/C797S-IN-1 以剂量依赖的方式抑制 P-EGFR 蛋白的表达。
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...
T36648	Tucatinib hemiethanolate
	Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ...

化合物

WHI-P180

Cat.No: T2032

Synonym: Janex 3

Target: EGFR, VEGFR, c-RET, CDK

WHI-P154

Cat.No: T1985

Synonym: Jak3 inhibitor ii

Target: Apoptosis, EGFR, VEGFR, JAK, Src

TD52

Cat.No: T35528

Synonym:

Target: Apoptosis, Phosphatase, Akt

Synonym: TD52 dihydrochloride(1798328-24-1 Free base),TD52 2HCl

Target: Others

EGFR-IN-1 hydrochloride

EGFR T790M/L858R-IN-2

Tucatinib hemiethanolate

Cat.No: T36648

Synonym:

Target:

Cat. No.	Product Name	Target	Signaling Pathways
TL0016	Sulforaphene 油菜	Apoptosis; ERK; EGFR; NF-κB	Angiogenesis; Apoptosis; JAK/STAT signaling; MAPK; NF-κB; Tyrosine Kinase/Adaptors
	Sulforaphene 是从萝卜种子中分离出来的天然产物，对鹿茸幼苗的 ED50 约为 2 x 10 -4 M。它通过抑制 EGFR、p-ERK1/2、NF-κB 和其他信号促进癌细胞凋亡并抑制迁移。

天然产物

Sulforaphene

Cat.No: TL0016

Synonym: 油菜

Target: Apoptosis, ERK, EGFR, NF-κB

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