892772-75-7
892772-75-7
Chemical Structure
EAI001
- No. CAS: 892772-75-7
- Formula:C19H15N3O2S
- Molecular Weight:349.41
IUPAC Name: 2-(1-oxoisoindolin-2-yl)-2-phenyl-N-(thiazol-2-yl)acetamide
InChIKey: PWRVRDCBFYLYFU-UHFFFAOYSA-N
SMILES: O=C(C(C1=CC=CC=C1)N2C(C(C=CC=C3)=C3C2)=O)NC4=NC=CS4
Biological Activity: EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer[1][2].
| Referencia número | Nombre del producto | Pureza | Descripciòn | Pricing | |||||||||||||||||||
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EAI001 | 99.93% | EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer. | ||||||||||||||||||||
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EAI001 (Standard) | ≥98% | EAI001 (Standard) is the analytical standard of EAI001 (HY-100214). This product is intended for research and analytical applications. EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer. | ||||||||||||||||||||
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EAI045 | 99.06% | EAI045 is an allosteric and the fourth-generation inhibitor of mutant EGFR with IC50s of 1.9, 0.019, 0.19 and 0.002 μM for EGFR, EGFRL858R, EGFRT790M and EGFRL858R/T790M at 10 μM ATP, respectively. | ||||||||||||||||||||
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CC-3052 | CC-3052 is a phosphodiesterase 4 (PDE4) inhibitor with immunomodulatory activities. CC-3052 reduces neutrophil apoptosis in HIV⁺. CC-3052 is promising for research of HIV-related diseases. | |||||||||||||||||||||
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LTβR-IN-1 | 99.79% | LTβR-IN-1 (Compound 919278) is a potent, selective lymphotoxin β receptor (LTβR) inhibitor. LTβR-IN-1 also selectively inhibits the nuclear translocation of p52 depended on TNF12A, instead of the nuclear translocation of p65 mediated by TNF-α receptor. LTβR-IN-1 regulates the NF-kB signaling pathway IN a ligand-independent manner. | ||||||||||||||||||||
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α-Phthalimidopropiophenone | 99.9% | α-Phthalimidopropiophenone is a drug derivative. | ||||||||||||||||||||
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JBJ-04-125-02 | JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities. | |||||||||||||||||||||
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(Rac)-JBJ-04-125-02 | (Rac)-JBJ-04-125-02 is the racemate of JBJ-04-125-02. JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor. | |||||||||||||||||||||
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JBJ-02-112-05 | JBJ-02-112-05 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 15 nM for EGFRL858R/T790M. | |||||||||||||||||||||
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JBJ-09-063 | JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer. | |||||||||||||||||||||
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GSK-3β inhibitor 11 | 98.02% | GSK-3β inhibitor 11 (compound 21) is a glycogen synthase kinase-3β (GSK-3β) inhibitor (IC50=10.02 μM). GSK-3β inhibitor 11 can be used in neurodegenerative disease research. | ||||||||||||||||||||
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JBJ-07-149 | 99.09% | JBJ-07-149 is an inhibitor for EGFRL858R/T790M with an IC50 of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC50 of 4.9 μM and 0.148 μM, without and with presence of Cetuximab (HY-P9905). JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163 (HY-139997). | ||||||||||||||||||||
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References
- [1]. Maity S, et, al. Advances in targeting EGFR allosteric site as anti-NSCLC therapy to overcome the drug resistance. Pharmacol Rep. 2020 Aug;72(4):799-813. [Content Brief]
- [2]. Tinivella A, et, al. Investigating the selectivity of allosteric inhibitors for mutant t790m egfr over wild type using molecular dynamics and binding free energy calculations. 2018 Dec 4;3(12):16556-62.
