| DC44893 |
Rezivertinib |
Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity. |
|
| DC45317 |
EGFR/ErbB-2/ErbB-4 inhibitor-2
Featured
|
EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM. |
|
| DC45794 |
Tucatinib hemiethanolate
Featured
|
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. |
|
| DC45832 |
Epitinib succinate |
Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer. |
|
| DC46163 |
Epitinib |
Epitinib is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib can be used for the research of cancer. |
|
| DC46170 |
EGFR-IN-16 |
EGFR-IN-16 (compound 3) is a potent EGFR inhibitor with pIC50 of 4.85 and 4.74 for EGFR and HER-2, respectively. |
|
| DC57050 |
DZD9008
Featured
|
DZD9008 is an oral, potent, irreversible, wild type-selective EGFR TKI against EGFR or HER2 Exon20ins and other mutations. |
|
| DC46219 |
EGFR mutant-IN-1 |
EGFR mutant-IN-1, a 5-methylpyrimidopyridone derivative, is a potent and selective EGFRL858R/T790M/C797S mutant inhibitor with an IC50 of 27.5 nM, while being a significantly less potent for EGFRWT (IC50 >1.0 μM). |
|
| DC46434 |
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. |
|
| DC46456 |
JNJ28871063 hydrochloride |
JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC50 values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2. |
|
| DC46464 |
BGB-102 |
BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively. |
|
| DC46929 |
Erlotinib-13C6 |
Erlotinib-13C6 (CP-358774-13C6) is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. |
|
| DC46930 |
Sunvozertinib |
Sunvozertinib is a potent ErbBs (EGFR, Her2, especially mutant forms) and BTK inhibitor. Sunvozertinib shows IC50s of 20.4, 20.4, 1.1, 7.5, and 80.4 nM for EGFR exon 20 NPH insertion, EGFR exon 20 ASV insertion, EGFR L858R and T790M mutations, and Her2 Exon20 YVMA, and EGFR WT A431, respectively (patent WO2019149164A1, example 52). |
|
| DC47115 |
Befotertinib |
Befotertinib (D-0316) is the third-generation EGFR tyrosine kinase inhibitor. Befotertinib can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC). |
|
| DC47271 |
Tyrphostin 8 |
Tyrphostin 8 is a tyrosine kinase, with an IC50 of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC50=21 μM). |
|
| DC47667 |
EGFR/CSC-IN-1 |
EGFR/CSC-IN-1 is a potential EGFR (IC50 10.52 nM) and cancer stem cell (CSC) dual inhibitor for triple-negative breast cancer treatment. |
|
| DC47668 |
EGFR-IN-17 |
EGFR-IN-17 is a potent and selective inhibitor of the epidermal growth factor receptor ( IC50 0.0002 μM) to overcome C797S-mediated resistance. |
|
| DC47669 |
EGFR-IN-18 |
EGFR-IN-18 potently inhibits enzymatic activity in L858R/T790M/C797S mutant EGFR (4.9 nM), with a significantly lower activity for wild-type EGFR (47 nM). |
|
| DC47902 |
SH-1028 mesylate |
SH-1028 (mesylate) is a selective and oral active inhibitor of EGFR with an IC50 of 18 nM. SH-1028 (mesylate) exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. SH-1028 (mesylate) significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation. |
|
| DC48361 |
Dosimertinib |
Dosimertinib is a highly potent, selective, and orally efficacious deuterated EGFR targeting clinical candidate for the treatment of non-small-cell lung cancer. |
|
| DC49109 |
EGFR-IN-24 |
EGFR-IN-24, a potent EGFR inhibitor, shows inhibition against EGFR(del19/T790M/C797S) and EGFR(L858R/T790M/C797S), respectively. |
|
| DC49127 |
Oritinib |
Oritinib (SH-1028), an irreversible third-generation EGFR TKI, overcomes T790M-mediated resistance in non-small cell lung cancer. Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFRWT, EGFRL858R, EGFRL861Q, EGFRL858R/T790M, EGFRd746-750 and EGFRd746-750/T790M kinases, with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively. |
|
| DC49160 |
EGFR-IN-25 |
EGFR-IN-25 is a potent EGFR inhibitor with IC50s of 9 nM and 60 nM for BaF3 cells (EGFR DEL19/T790M/C797S) and A431 cells (WT), respectively. |
|
| DC49163 |
EGFR-IN-27 |
EGFR-IN-27 is a potent EGFR inhibitor with IC50s of <50 nM for EGFR Del, L858R, Del/T790M, L858R/T790M, Del/T790M/C797S, and L858R/T790M/C797S, respectively (WO2021249324A1, compound 511). |
|
| DC49172 |
EGFR-IN-21 |
EGFR-IN-21 is a potent EGFR inhibtior with an IC50 of 0.38 nM. EGFR-IN-21 has antitumor activity. |
|
| DC49173 |
EGFR-IN-23 |
EGFR-IN-23 is a potent EGFR TKI (tyrosine kinase inhibitor) with an IC50 of 8.05 nM for BaF3/EGFR-DEL19/T790M/C797S cell (WO2021244502A1, compound 8). |
|
| DC49188 |
EGFR-IN-22 |
EGFR-IN-22 is a potent EGFR inhibitor with IC50s of 4.91 nM and 0.54 nM for wild type EGFR and EGFRL858R/T790M/C797S, respectively (CN112538072A, compound 243). |
|
| DC50095 |
EGFR-IN-34 |
EGFR-IN-34 is a potent inhibitor of EGFR. EGFR-IN-34 is an anti-tumor drug with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-34 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 12). |
|
| DC50097 |
(E)-AG 556 |
(E)-AG 556 is a highly selective EGFR inhibitor and also blocks LPS-induced TNF-α production. |
|
| DC50100 |
EGFR-IN-29 |
EGFR-IN-29 is a potent EGFR inhibitor, example J-022, extracted from Patent WO2021160087. |
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