| Cat. No. |
Product Name |
Information |
| PC-24129 |
Emupertinib
EGFR inhibitor
|
Emupertinib (TAS3351) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively |
| PC-23725 |
ERBB4 agonist EF-1
ERBB4 agonist
|
ERBB4 agonist EF-1 is a specific small molecule ERBB4 (HER4) agonist that induce ERBB4 homodimerization with EC50 of 10.5 uM in ERBB4/ERBB4 dimerization assay, reduces cell death and hypertrophy in cardiomyocytes and decreases collagen production in cardiac fibroblasts. |
| PC-23314 |
BAY 2476568
EGFR Ex20Ins inhibitor
|
BAY 2476568 (BAY-598) is the first reversible, potent and selective inhibitor of EGFR exon 20 insertions with IC50 of 20 and 24 nM for V769_D770insASV (insASV) and D770_N771insSVD (insSVD), with a wide margin of selectivity versus WT EGFR. |
| PC-23313 |
TAK-285
HER2/EGFR inhibitor
|
TAK-285 (TAK285) is a potent, dual inhibitor of HER2 and EGFR (HER1) with IC50 of 17 nM and 23 nM, respectively. |
| PC-22758 |
MTX-531
EGFR/PI3K inhibitor
|
MTX-531 (MTX531) is a first-in-class, potent and selective inhibitor of EGFR and PI3K with IC50 of 15 nM and 6.4 nM (PI3Kα), respectively. |
| PC-22307 |
Mefatinib
EGFR inhibitor
|
Mefatinib (Mifanertinib dimaleate, MET306, MET-306) is a potent, bioavailable, second-generation, irreversible dual inhibitor of EGFR/HER2 with IC50 of 0.4/11.7 nM, respectively. |
| PC-21782 |
HSL119
HUNK inhibitor
|
HSL119 (HSL-119) is a potent and selective hormonally upregulated neu-associated kinase (HUNK) inhibitor, completely inhibits HUNK kinase activity at 1 uM in biochemical assays. |
| PC-21761 |
BI-4732
EGFR inhibitor
|
BI-4732 is a potent, highly BBB penetrant, fourth-generation EGFR inhibitor against EGFR activating mutations with IC50 of <1 nM for EGFR L858R, T790M and C797S. |
| PC-21566 |
BDTX-1535
EGFR inhibitor
|
Silevertinib (BDTX-1535) is a 4th generation, irreversible, CNS penetrant, potent, wild type sparing EGFR inhibitor, targets a family of oncogenic EGFR extracellular domain alterations and amplification in GBM, and EGFR resistance mutations in NSCLC. |
| PC-21322 |
STX-721
EGFR inhibitor
|
Elticertinib (STX-721) is a potent, selective, irreversible, orally active inhibitor of EGFR/HER2 ex20ins mutants with IC50 of 5.4 nM and 5.8 nM for cellular Ba/F3 EGFR ex20insASV and insSVD mutant activity, respectively. |
| PC-21212 |
MTX-241F
EGFR/PI3K inhibitor
|
MTX-241F (MTX241F) is a potent, highly selective and brain-penetrant inhibitor of EGFR, PI3K and DNA-PK with IC50 of 3 nM, 87 nM (PI3Kα) and 5.5 nM, respectively. |
| PC-20781 |
Mubritinib
HER2 inhibitor
|
Mubritinib (TAK-165) is a potent inhibitor of human epidermal growth factor receptor 2 (HER2, ERBB2) tyrosine kinase with IC50 of 6 nM, also is a potent Complex I inhibitor with IC50 of 51 nM. |
