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Search Results for " egfr-in-50 "

16

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T63996	EGFR-IN-50
	EGFR-IN-50 是一种针对 L858R 抗性突变的强效 EGFR 抑制剂，能够作用于 TEL-EGFR-L858R-BaF3 及 TEL-EGFR-T790M-L858R-BaF3，他们的 GI50 值分别为 8 nM、6.03 μM。EGFR-IN-50 对癌细胞表现出抗增殖作用。
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 ...
T60729	EGFR-IN-67
	EGFR-IN-67 (Compound 7d) 是具有抗癌活性的EGFR 抑制剂 (IC 50 = 0.34 μM)。
T61225	EGFR-IN-64
	EGFR-IN-64 (Compound 3c) is a highly potent inhibitor of the epidermal growth factor receptor (EGFR) with an IC 50 value of 0.33 μM. This compound, EGFR-IN-64, exhibits significant anticancer activity [1].
T40785	Gefitinib impurity 1
	Gefitinib impurity 1 is a compound derived from Gefitinib, a potent and selective EGFR tyrosine kinase inhibitor (IC 50 = 33 nM). This orally active compound selectively inhibits tumor cell growth stimulated by EGF (IC 50 = 54 nM) and inhibits EGFR autophosphorylation induced by EGF in tumor cells. Additionally, Gefitinib induces autophagy and exhibits antitumor activity.
T83691	EGFR Peptide (human, mouse) TFA Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH,Epidermal Growth Factor Receptor Peptide
	EGFR peptide是一种PKC的多肽底物，其氨基酸序列与EGFR的细胞内区域相对应。它已被用于监测原代牛视网膜内皮细胞中的PKC活性。与EGFR peptide (myristoylated)不同，在50 µM浓度下使用时，EGFR peptide不会抑制PKC。
T1181L	Gefitinib hydrochloride
	Gefitinib hydrochloride (ZD1839 hydrochloride) 是一种有效，选择性和具有口服活性的EGFR 酪氨酸激酶抑制剂，IC50为 33 nM。Gefitinib hydrochloride 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC50为 54 nM)，并阻断 EGF 刺激的肿瘤细胞中EGFR 自磷酸化。Gefitinib hydrochloride 也诱导细胞自噬 (autophagy)，具有抗肿瘤活性。
T73154	EGFR-IN-70
	EGFR-IN-70 是一种有效的EGFR 抑制剂，对于EGFRLR/TM/CS 和EGFRWT，其IC50值分别为 23.6 和 307.5 nM。EGFR-IN-70 具有抗增殖活性并抑制EGFR 的磷酸化。EGFR-IN-70 可用于癌症研究。
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。
T72431	Theliatinib tartrate Xiliertinib tartrate,HMPL-309 tartrate,Xiliertinib tartrate ; HMPL-309 tartrate
	Theliatinib (Xiliertinib) tartrate 是一种有效、ATP 竞争性、口服活性和高度选择性的EGFR 抑制剂，Ki 为 0.05 nM，IC50为 3 nM。Theliatinib 对EGFRT790M/L858R 突变体的IC50值为 22 nM。Theliatinib 对EGFR 的选择性是其他激酶的 50 倍以上。
T41155	MS 154
	MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioa...
T35147	WZ4002-hydroxy WZ4002 analog, WZ4002 demethyl derivate,WZ 4002-hydroxy,WZ-4002-hydroxy
	WZ4002-hydroxyl is a WZ4002 derivative or WZ4002 analogue in which methoxy is replaced by hydroxyl and can be detected in 50% of patients with clinical resistance to gefitinib or erlotinib. WZ4002 has a basic chemical skeleton (covalent pyrimidine) that d
T36251	DP-C-4	PROTACs	PROTAC
	DP-C-4 is a Cereblon-based dual PROTAC for simultaneous degradation of EGFR and PARP[1]. DP-C-4 (1-50 μM; 24 hours) has degradation effects on EGFR and PARP simultaneously in a dose-dependent manner in SW1990 cells[1]. [1]. Mengzhu Zheng, et al. Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP. J Med Chem. 2021 May 26.
T36193	CAY10717
	CAY10717 is a multi-targeted kinase inhibitor that exhibits greater than 40% inhibition of 34 of 104 kinases in an enzymatic assay at a concentration of 100 nM. It has activity at multiple oncogenic kinases, with IC50 values less than 50 nM against wild-type EGFR and ABL and mutant ABLG250E, ABLY253F, ABLE255K, and B-RafV600E. CAY10717 is highly cytotoxic against a cancer cell panel that includes chemotherapy-sensitive and -resistant cell lines (EC50s = 0.4-158 nM). It also inhibits the growth o...
T35423	7-oxo Staurosporine
	7-oxo Staurosporine is an antibiotic originally isolated from S. platensis with diverse biological activites. It inhibits PKC, PKA, phosphorylase kinase, EGFR, and c-Src in vitro (IC50s = 9, 26, 5, 200, and 800 nM, respectively). 7-oxo Staurosporine induces cell cycle arrest in the G2/M phase in human leukemia K562 cells with a minimal effective dose (MED) of 30 ng/ml. It is cytotoxic to P388 mouse leukemia cells that are resistant and susceptible to doxorubicin . 7-oxo Staurosporine inhibits gr...
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

Cat.No: T63996

Tucatinib hemiethanolate

Cat.No: T36648

Cat.No: T60729

Cat.No: T61225

Gefitinib impurity 1

Cat.No: T40785

EGFR Peptide (human, mouse) TFA

Cat.No: T83691

Synonym: Arg-Lys-Arg-Thr-Leu-Arg-Arg-Leu-OH,Epidermal Growth Factor Receptor Peptide

Gefitinib hydrochloride

Cat.No: T1181L

Cat.No: T73154

EGFR/C797S-IN-1

Cat.No: T72788

Theliatinib tartrate

Cat.No: T72431

Synonym: Xiliertinib tartrate,HMPL-309 tartrate,Xiliertinib tartrate ; HMPL-309 tartrate

Cat.No: T41155

Cat.No: T35147

Synonym: WZ4002 analog, WZ4002 demethyl derivate,WZ 4002-hydroxy,WZ-4002-hydroxy

Cat.No: T36251

Target: PROTACs

Cat.No: T36193

7-oxo Staurosporine

Cat.No: T35423

Cat.No: T35897

Cat. No.	Product Name	Target	Signaling Pathways
TN3525	Boehmenan	ERK; Phosphatase; EGFR; PARP; MEK; Wnt/beta-catenin; Akt; Caspase; STAT; p53	Angiogenesis; Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Metabolism; PI3K/Akt/mTOR signaling; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors
	(±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity in a competitive manner. Boehmenan exhibits the potent cytotoxic effects against many cancer cell

天然产物

Cat.No: TN3525

Target: ERK, Phosphatase, EGFR, PARP, MEK, Wnt/beta-catenin, Akt, Caspase, STAT, p53

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