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Cat No. | Product Name | Synonyms | Targets |
---|---|---|---|
T63732 | EGFR-IN-3 | Apoptosis , EGFR | |
EGFR-IN-3 is an EGFR inhibitor with potential antitumour activity.EGFR-IN-3 inhibits EGFRwt-TK and induces apoptosis (cell death), which can cause cells to block in the G2/M phase. | |||
TQ0255 | Olafertinib | CK-101,EGFR-IN-3,RX-518 | EGFR |
Olafertinib (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC. | |||
T12131 | Mutated EGFR-IN-3 | EGFR | |
Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) inhibitor(IC50 of 12 nM and 13 nM, respectively. ) | |||
T62777 | EGFR/HER2-IN-3 | ||
EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual EGFR and HER2 inhibitor. | |||
T79394 | ALK/EGFR-IN-3 | ||
ALK/EGFR-IN-3 is a dual ALK and EGFR inhibitor that demonstrates potent anti-proliferative effects on various cancer cell lines, including H1975, PC9, and Baf3-EML4-ALK, with respective IC50 values of 0.1360, 0.0332, and... | |||
T79728 | EGFR/CDK2-IN-3 | EGFR | |
EGFR/CDK2-IN-3 (compound 4b) serves as a dual inhibitor targeting both EGFR and CDK-2, exhibiting IC50 values of 71.7 nM and 113.7 nM, respectively. It prompts apoptosis in MCF-7 cells and halts the cell cycle in the S p... | |||
T78850 | EGFR/BRAFV600E-IN-3 | EGFR | |
EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively. It induces apoptosis and exhibits promising antioxidant activity [1]. | |||
T63161 | EGFR/HER2/CDK9-IN-3 | ||
EGFR/HER2/CDK9-IN-3 (Compound 10) is a potent inhibitor of EGFR (IC50:191.08 nM), HER2 (IC50:132.65 nM), and CDK9 (IC50:113.98 nM). EGFR/HER2/CDK9-IN-3 showed significant anti-tumor effects. | |||
T82492 | EGFR/HER2/DHFR-IN-3 | EGFR | |
EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.092 μM for HER2, respectively. Moreover, it demonstrates inhi... | |||
T5437 | Gefitinib-based PROTAC 3 | EGFR | |
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectivel... | |||
T4657L | WHI-P97 HCl 211555-05-4(free base) | JAK | |
WHI-P97 HCl is a potent and selective JAK-3 inhibitor. WHI-P97 had an estimated Ki value of 0.09 microM from modeling studies and a measured IC50 value of 2.5 microM in EGFR kinase inhibition assays. WHI-P97 effectively ... | |||
TJS0339 | Coumarin-3-carboxylic acid | 3-Carboxycoumarin | VEGFR |
The combination of Valproic acid with Coumarin-3-carboxylic acid (3-Carboxycoumarin) suppresses the proliferation and migration of lung cancer cells via EGFR/VEGFR2/c-Met-Akt-NF-κB signaling pathways; this combination ma... | |||
T74351 | PROTAC EGFR degrader 3 | ||
PROTAC EGFR Degrader 3, a highly potent molecule, exhibits remarkable cellular activity against H1975 and HCC827 cells, maintaining high selectivity. It additionally reveals the lysosome's crucial role in the degradation... | |||
T72431 | Theliatinib tartrate | Xiliertinib tartrate,HMPL-309 tartrate,Xiliertinib tartrate ; HMPL-309 tartrate | |
Theliatinib (Xiliertinib) tartrate is a potent and highly selective EGFR inhibitor, displaying ATP-competitive and orally active properties. It exhibits promising efficacy with a K_i of 0.05 nM and an IC_50 of 3 nM for E... | |||
T62681 | PDE5-IN-3 | ||
PDE5-IN-3 (compound 11j) is a potent inhibitor of PDE5 (IC50: 1.57 nM). PDE5-IN-3 has a moderate inhibitory effect on EGFR (IC50: 5.827 μM). PDE5-IN-3 markedly inhibits the Wnt/β-catenin pathway with an IC50 value of 128... | |||
T82493 | EGFR/HER2/DHFR-IN-2 | EGFR | |
EGFR/HER2/DHFR-IN-2 (Compound 4b) serves as an inhibitor for EGFR, HER2, and DHFR, with IC50 values of 0.248, 0.156, and 0.138 μM, respectively. It exhibits anticancer activity, displaying IC50 values of 9.14, 7.33, 14.1... | |||
T28874 | SU11652 | SU-11652,SU 11652 | |
SU11652 is a potent cell-permeable pyrrole-indolinone compound. SU11652 acts as an ATP-competitive tyrosine kinase receptor and angiogenic inhibitor with greater selectivity for PDGFR-β (PDGFRβ, IC50 = 3 nM), Flk-1 (VEGF... | |||
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... | |||
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-f... | |||
T76721 | Zalutumumab | ||
Zalutumumab, a fully human IgG1 monoclonal antibody, exhibits high affinity for the epidermal growth factor receptor (EGFR), selectively targeting its domain III. It functions by inhibiting the binding of the epidermal g... |