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Cat No. | Product Name | Synonyms | Targets |
---|---|---|---|
T11164 | EGFR mutant-IN-1 | EGFR | |
EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R/T790M/C797S mutant inhibitors with IC50 of 27.5 nM, which significantly weakened EGFRWT effect. | |||
T11157L | EGFR-IN-1 hydrochloride | EGFR | |
EGFR-IN-1 hydrochloride is an irreversible and specific inhibitor of L858R/T790M mutant EGFR with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 hydrochloride exhibits potent antitumor and antiproliferative activity... | |||
T16162 | Mutated EGFR-IN-1 | Osimertinib analog | EGFR |
Mutated EGFR-IN-1 (Osimertinib analog) is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant, and T790M resistance mutant. | |||
T10534 | BI-4020 | EGFR | |
BI-4020 is a fourth-generation, orally active, and non-covalent inhibitor of EGFR tyrosine kinase. BI-4020 exhibits activity agains the triple mutant EGFR del19 T790M C797S variant (IC50=0.2 nM in BaF3 cell lines), the d... | |||
T61016 | EMI1 | EGFR | |
EMI1 can be used in the mutant EGFR-associated, drug-resistant non-small-cell lung cancer(NSCLC) research. EMI1 is an inhibitor of EGFR L858R/T790M/C797S and EGFR ex19del/T790M/C797S [1]. | |||
T11157 | EGFR-IN-1 | EGFR | |
EGFR-IN-1, an orally active and irreversible selective inhibitor targeting L858R/T790M mutant EGFR, exhibits strong antiproliferative and antitumor activity, particularly against H1975 cells and first line mutant HCC827 ... | |||
T75261 | EGFR-IN-1 TFA | ||
EGFR-IN-1 TFA is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 TFA potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR . EGFR-I... | |||
T74561 | JBJ-09-063 TFA | ||
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor, displaying IC50 values of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R/T790M, 0.083 nM for EGFR L858R/T790M/C797S, and 0.396 nM for EGFR L747S mutations... | |||
T74351 | PROTAC EGFR degrader 3 | PROTACs | |
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... | |||
T77073 | Losatuxizumab | ||
Losatuxizumab (ABT-806), an anti-EGFR monoclonal antibody, exhibits selective binding affinity towards various EGFR forms, with EC50 values of 0.96 nM for the wild-type EGFR, 0.09 nM for the C271A,C283A mutant, 0.12 nM f... | |||
T79775 | EGFR-IN-89 | EGFR | |
EGFR-IN-89 (compound 13k) is a fourth-generation inhibitor selectively targeting EGFR mutations, exhibiting potent activity with an IC50 of 10.1 nM against Del19/T790M/C797S mutations, and demonstrating greater selectivi... | |||
T79461 | YK-029A | EGFR | |
YK-029A, an orally active EGFR mutant inhibitor, targets both EGFR T790M and EGFRex20ins mutations. It demonstrates notable antitumor efficacy, inducing tumor regression in EGFRex20ins-driven patient-derived xenograft (P... | |||
T74633 | MS9427 | ||
MS9427 is a potent PROTAC EGFR degrader, demonstrating high affinity for EGFR with dissociation constants (K d s) of 7.1 nM for the wild-type (WT) EGFR and 4.3 nM for the L858R mutant EGFR, indicating selective degradati... | |||
T80748 | YS-363 | EGFR | |
YS-363 is a potent, selective, and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting half-maximal inhibitory concentrations (IC50) of 0.96 nM for the wild-type EGFR and 0.67 nM for the ... | |||
T74635 | MS9449 | PROTACs | |
MS9449 is a potent PROTAC EGFR degrader, exhibiting dissociation constants (Kd) of 17 nM for EGFR WT and 10 nM for EGFR L858R. It effectively mediates the degradation of mutant EGFRs via both ubiquitin/proteasome system ... | |||
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]... | |||
T74634 | MS9427 TFA | PROTACs | |
MS9427 TFA is a potent PROTAC-based EGFR degrader, exhibiting dissociation constants (Kd) of 7.1 nM for wild-type EGFR and 4.3 nM for the L858R EGFR mutation. It preferentially degrades the mutant EGFR, sparing the wild-... |