Shopping Cart
- Remove All
Your shopping cart is currently empty
ES-072
😃Good
Catalog No. T200087Cas No. 2089721-94-6
ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.
ES-072
😃Good
Catalog No. T200087Cas No. 2089721-94-6
ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks |
Bulk & Custom
Add to Cart
Questions
View MoreInhibitors Related to "ES-072"
Gefitinib
Cited
ZD1839
T1181184475-35-2
Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation.
- $50
Size
QTY
CitedErlotinib Cited
R1415, OSI-744, NSC 718781, CP358774
T0373183321-74-6
Erlotinib (NSC-718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
- $40
Size
QTY
CitedOsimertinib Cited
Mereletinib, AZD-9291
T24901421373-65-0
Osimertinib (AZD-9291) is an EGFR third-generation inhibitor that inhibits the T790M resistance mutation produced by second-generation EGFR inhibitors with irreversible and oral activity. Osimertinib has antitumor activity for the treatment of EGFR-mutated non-small-cell lung cancer.
- $32
Size
QTY
CitedLapatinib Cited
GW572016, GSK572016
T0078231277-92-2
Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2/10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.
- $29
Size
QTY
CitedNeratinib Cited
HKI-272
T2325698387-09-6
Neratinib (HKI-272) (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively.
- $30
Size
QTY
CitedGenistein Cited
NPI 031L
T1737446-72-0
Genistein (NPI 031L) is a naturally occurring soy isoflavone, a multi-targeted tyrosine kinase inhibitor. Genistein has antitumor, antioxidant, and anthelmintic properties, and also produces estrogen-like effects in the body.
- $38
Size
QTY
CitedErlotinib hydrochloride
OSI-744, NSC 718781, Erlotinib HCl, CP-358774
T0373L183319-69-9
Erlotinib hydrochloride (NSC 718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
- $35
Size
QTY
Lidocaine Hydrochloride hydrate
T1144L6108-05-0
Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.
- $32
Size
QTY
Chalcone
β-phenylacrylophenone, phenyl styryl ketone, Cinnamophenone, benzylideneacetophenone, benzalacetophenone
T2S096194-41-7
Chalcone (Cinnamophenone) is an aromatic ketone that forms the central core for a variety of important biological compounds, which are known collectively as chalcones.
- $31
Size
QTY
4-Chloro-2'-bromoacetophenone
T8908536-38-9
4-Chloro-2'-bromoacetophenone against glycogen synthase kinase-3 (GSK-3beta).
- $30
Size
QTY
CHIR-99021 Cited
Laduviglusib, CT99021, CHIR-99021
T2310252917-06-9
CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.
- $36
Size
QTY
CitedAfatinib Dimaleate Cited
BIBW2992, BIBW 2992MA2, Afatinib (BIBW2992) Dimaleate, Afatinib
T1773850140-73-7
Afatinib Dimaleate (BIBW 2992MA2) is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity.
- $34
Size
QTY
CitedContact us for more batch information
Resource Download
Product Introduction
Bioactivity
Chemical Properties
| Description | ES-072, a selective inhibitor targeting the EGFR mutant (EGFR-T790M), is administered orally. By hindering EGFR-T790M activity, it activates GSK3α, which subsequently leads to the phosphorylation of PD-L1 at Ser279 and Ser283. This phosphorylation facilitates the recruitment of the E3 ubiquitin ligase ARIH1, resulting in the ubiquitination and proteasomal degradation of PD-L1. Such a process not only curtails the growth of cancer cells but also amplifies the anti-tumor immune response by diminishing PD-L1 levels. ES-072 has shown efficacy in impeding the proliferation of non-small cell lung cancer (NSCLC) cells. |
| Molecular Weight | 528.53 |
| Formula | C25H27F3N8O2 |
| Cas No. | 2089721-94-6 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Preview
Related Tags: buy ES-072 | purchase ES-072 | ES-072 cost | order ES-072 | ES-072 chemical structure | ES-072 formula | ES-072 molecular weight
- TOP
Feedback
Hello! How can I help you today? 
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.