Product Name |
EGFR/ErbB1/HER1 |
ErbB2/HER2 |
ErbB3/HER3 |
ErbB4/HER4 |
Purity |
Osimertinib |
EGFRL858R, IC50: 12 nM (Enzyme assays)
EGFRL858R/T790M, IC50: 1 nM (Enzyme assays)
|
|
|
|
99.96% |
Trastuzumab |
|
|
|
|
99.80% |
Gefitinib |
|
|
|
|
99.94% |
Cetuximab |
Soluble EGFR, Kd: 0.201 nM
EGFR, Kd: 0.147 nM (Fixed A431 cells)
|
|
|
|
99.70% |
Erlotinib |
EGFR, IC50: 2 nM (Cell Free Assay)
|
|
|
|
99.99% |
Afatinib |
EGFR, IC50: 0.5 nM
EGFRL858R, IC50: 0.4 nM
EGFRL858R/T790M, IC50: 10 nM
|
|
|
|
99.92% |
Lapatinib |
EGFR, IC50: 10.2 nM (Cell Free Assay)
|
ErbB2, IC50: 9.8 nM (Cell Free Assay)
|
|
|
99.83% |
Genistein |
EGFR, IC50: 0.6 μM (Cell Assay)
|
|
|
|
99.86% |
AG490 |
|
|
|
|
99.92% |
Tucatinib |
|
|
|
|
99.82% |
Neratinib |
|
|
|
|
99.94% |
Disitamab vedotin |
|
|
|
|
≥99.0% |
Dacomitinib |
|
|
|
|
99.74% |
AG-1478 |
|
|
|
|
99.22% |
Pertuzumab |
|
|
|
|
99.80% |
Osimertinib mesylate |
EGFRL858R/T790M, IC50: 1 nM
EGFRL858R, IC50: 12 nM
|
|
|
|
99.97% |
NSC 228155 |
|
|
|
|
≥98.0% |
Erlotinib Hydrochloride |
|
|
|
|
99.93% |
Lazertinib |
|
|
|
|
99.07% |
Sapitinib |
|
|
|
|
99.93% |
Mobocertinib |
EGFR (WT)
EGFR exon 20 insertion
|
|
|
|
99.60% |
Almonertinib |
EGFRT790M, IC50: 0.37 nM
EGFRL858R/T790M, IC50: 0.29 nM
EGFRdel19 T790M, IC50: 0.21 nM
|
|
|
|
99.98% |
Firmonertinib mesylate |
|
|
|
|
99.97% |
Pyrotinib |
|
|
|
|
99.89% |
Icotinib |
|
|
|
|
99.99% |
CUDC-101 |
|
|
|
|
98.84% |
Afatinib dimaleate |
EGFR, IC50: 0.5 nM
EGFRL858R, IC50: 0.4 nM
EGFRL858R/T790M, IC50: 10 nM
|
|
|
|
99.88% |
Daphnetin |
|
|
|
|
99.86% |
Gefitinib hydrochloride |
|
|
|
|
99.85% |
Lifirafenib |
EGFR, IC50: 29 nM
EGFRL858R/T790M, IC50: 495 nM
|
|
|
|
98.73% |
Canertinib |
|
|
|
|
99.82% |
Chrysophanol |
|
|
|
|
99.77% |
Pelitinib |
|
|
|
|
98.80% |
TX1-85-1 |
|
|
|
|
98.04% |
Butein |
EGFR, IC50: 16 μM (in HepG2 cells)
|
|
|
|
99.95% |
Zanidatamab |
|
|
|
|
|
Mubritinib |
|
|
|
|
99.91% |
Olmutinib |
EGFRExon 19 deletion, IC50: 9.2 nM (Cell Assay)
EGFRL858R/T790M, IC50: 10 nM (Cell Assay)
|
|
|
|
99.88% |
Osimertinib dimesylate |
EGFRL858R, IC50: 12 nM
EGFRL858R/T790M, IC50: 1 nM
|
|
|
|
99.96% |
Sunvozertinib |
EGFR exon 20 insertion, IC50: 20.4 nM
EGFRL858R/T790M, IC50: 1.1 nM
|
Her2 Exon20 YVMA, IC50: 7.5 nM
|
|
|
99.92% |
PD153035 |
EGFR, Ki: 6 pM
EGFR, IC50: 25 pM
|
|
|
|
98.83% |
Lapatinib ditosylate |
EGFR, IC50: 10.8 nM (Cell Free Assay)
|
ErbB2, IC50: 9.2 nM (Cell Free Assay)
|
|
|
99.98% |
EAI045 |
EGFR, IC50: 1.9 μM
EGFRL858R, IC50: 0.019 μM
EGFRT790M, IC50: 0.19 μM
EGFRL858R/T790M, IC50: 0.002 μM
|
|
|
|
99.08% |
Zorifertinib |
EGFR, IC50: 0.3 nM
EGFRL858R, IC50: 0.2 nM
EGFRExon 19 deletion, IC50: 0.2 nM
|
|
|
|
99.76% |
Gefitinib-based PROTAC 3 |
EGFR, DC50: 11.7 nM (HCC827(exon 19 del) cells)
EGFR, DC50: 22.3 nM (H3255 (L858R mutantion) cells)
|
|
|
|
99.98% |
Rociletinib |
EGFRL858R/T790M, Ki: 21.5 nM
EGFRT790M, Ki: 303.3 nM
|
|
|
|
99.79% |
Pertuzumab (anti-HER2) |
|
|
|
|
99.10% |
Tesevatinib |
|
|
|
|
99.21% |
Pyrotinib dimaleate |
|
|
|
|
98.56% |
AZ-5104 |
EGFRL858R/T790M, IC50: 1 nM
EGFRL858R, IC50: 1 nM
EGFRL861Q, IC50: 6 nM
EGFR, IC50: 25 nM
|
|
|
|
99.70% |
CP-724714 |
|
|
|
|
98.53% |
Tyrphostin 23 |
EGFR, IC50: 35 μM (Cell Assay)
EGFR, Ki: 11 μM
|
|
|
|
99.43% |
BMS-690514 |
|
|
|
|
99.07% |
BI-4020 |
EGFRdel19 T790M C797S, IC50: 0.2 nM
EGFRdel19, IC50: 1 nM
EGFRWT, IC50: 190 nM
|
|
|
|
99.28% |
Disitamab |
|
|
|
|
|
PD168393 |
|
|
|
|
98.58% |
Zipalertinib |
|
|
|
|
99.81% |
Icotinib Hydrochloride |
|
|
|
|
99.81% |
Avitinib |
EGFR L858R, IC50: 0.18 nM
EGFRT790M, IC50: 0.18 nM
EGFR (WT), IC50: 7.68 nM
|
|
|
|
99.90% |
Varlitinib |
|
|
|
|
98.03% |
PD158780 |
EGFR, IC50: 8 μM (Cell Assay)
|
ErbB2, IC50: 49 nM (Cell Assay)
|
ErbB3, IC50: 52 nM (Cell Assay)
|
ErbB4, IC50: 52 nM (Cell Assay)
|
99.56% |
Petosemtamab |
|
|
|
|
|
AEE788 |
|
|
|
|
99.13% |
WZ4002 |
EGFRL858R, IC50: 2 nM (Cell Assay)
EGFRL858R/T790M, IC50: 8 nM (Cell Assay)
EGFRE746_A750, IC50: 3 nM (Cell Assay)
EGFRE746_A750/T790M, IC50: 2 nM (Cell Assay)
|
|
|
|
99.76% |
TAK-285 |
|
|
|
|
99.70% |
AG-825 |
|
|
|
|
98.02% |
Nazartinib |
EGFRL858R/T790M, Ki: 31 nM
|
|
|
|
99.03% |
JBJ-09-063 hydrochloride |
EGFR L858R, IC50: 0.147 nM
EGFR L858R/T790M, IC50: 0.063 nM
EGFR L858R/T790M/C797S, IC50: 0.083 nM
EGFRLT/L747S, IC50: 0.396 nM
|
|
|
|
99.37% |
Rezivertinib |
|
|
|
|
99.43% |
Tuxobertinib |
|
|
|
|
99.90% |
Lumretuzumab |
|
|
|
|
≥99.0% |
Falnidamol |
|
|
|
|
99.05% |
Lapatinib ditosylate monohydrate |
|
|
|
|
99.93% |
Allitinib tosylate |
EGFR, IC50: 0.5 nM
EGFRL858R/T790M, IC50: 12 nM
|
|
|
|
99.83% |
Genistein (Standard) |
|
|
|
|
99.31% |
WZ-3146 |
EGFRL858R, IC50: 2 nM
EGFRL858R/T790M, IC50: 5 nM
EGFRE746_A750, IC50: 2 nM
EGFRE746_A750/T790M, IC50: 14 nM
EGFR, IC50: 24 nM
|
|
|
|
99.63% |
Avitinib maleate |
EGFR (WT), IC50: 7.68 nM
EGFR L858R, IC50: 0.18 nM
EGFRT790M, IC50: 0.18 nM
|
|
|
|
≥98.0% |
Canertinib dihydrochloride |
|
|
|
|
99.68% |
WHI-P154 |
|
|
|
|
99.39% |
Naquotinib mesylate |
EGFRL858R/T790M
EGFRL858R
EGFRExon 19 deletion
EGFRExon 19 deletion/T790M
EGFR, IC50: 230 nM
|
|
|
|
98.05% |
Mutated EGFR-IN-1 |
EGFRL858R
EGFRExon 19 deletion/T790M
EGFRT790M
|
|
|
|
99.84% |
Epertinib hydrochloride |
EGFR, IC50: 1.48 ± 0.0 nM
|
|
|
HER4, IC50: 2.49 ± 0.1 nM
|
98.25% |
MTX-211 |
|
|
|
|
99.81% |
Neratinib maleate |
|
|
|
|
99.83% |
Almonertinib hydrochloride |
EGFRT790M, IC50: 0.37 nM
EGFRL858R/T790M, IC50: 0.29 mM
EGFRdel19 T790M, IC50: 0.214 nM
|
|
|
|
99.77% |
Myristicin |
|
|
|
|
99.89% |
VEGFR-IN-1 |
|
|
|
|
98.42% |
Tarloxotinib bromide |
|
|
|
|
99.26% |
CL-387785 |
|
|
|
|
98.05% |
Mobocertinib succinate |
EGFR exon 20 insertion
EGFR (WT)
|
|
|
|
99.83% |
limertinib |
EGFRT790M, IC50: 0.5 nM
EGFRL858R/T790M, IC50: 0.3 nM
EGFR (WT), IC50: 6 nM
EGFRExon 19 deletion, IC50: 0.5 nM
|
|
|
|
99.12% |
BI-4142 |
|
|
|
|
98.39% |
Simotinib |
|
|
|
|
99.39% |
(Rac)-JBJ-04-125-02 |
EGFR (L858R/T790M), IC50: 0.26 nM
|
|
|
|
|
MS154 |
EGFR (WT), Kd: 1.8 nM
EGFRL858R, Kd: 3.8 nM
|
|
|
|
99.42% |
HKI-357 |
|
|
|
|
99.65% |
Tarlox-TKI |
|
|
|
|
98.84% |
HG-14-10-04 |
EGFRLR/TM, IC50: 15.6 nM
EGFR19del/TM/CS, IC50: 22.6 nM
EGFRLR/TM/CS, IC50: 124.5 nM
|
|
|
|
99.09% |
EGFR/ErbB-2/ErbB-4 inhibitor-3 |
ErbB1, IC50: 0.3 nM
EGFR, IC50: 2.5 nM
|
|
|
|
98.19% |
Bafisontamab |
|
|
|
|
|
PD153035 Hydrochloride |
EGFR, Ki: 6 pM
EGFR, IC50: 25 pM
|
|
|
|
99.48% |
Naquotinib |
|
|
|
|
98.71% |
BI-1622 |
|
|
|
|
98.97% |
JBJ-09-063 TFA |
EGFR L858R, IC50: 0.147 nM
EGFR L858R/T790M, IC50: 0.063 nM
EGFR L858R/T790M/C797S, IC50: 0.083 nM
EGFRLT/L747S, IC50: 0.396 nM
|
|
|
|
99.64% |
Larotinib mesylate hydrate |
EGFR (WT), IC50: 0.611 nM
EGFRL858R, IC50: 0.563 nM
EGFRL861Q, IC50: 0.423 nM
EGFRT790M, IC50: 45.2 nM
|
|
|
|
98.66% |
Oritinib |
EGFR (WT), IC50: 18 nM
EGFRL858R, IC50: 0.7 nM
EGFRL861Q, IC50: 4 nM
EGFRL858R/T790M, IC50: 0.1 nM
EGFRd746-750, IC50: 1.4 nM
EGFRd746-750/T790M, IC50: 0.89 nM
|
|
|
|
99.18% |
PF-6274484 |
EGFR (WT), Ki: 0.18 nM
EGFRL858R/T790M, Ki: 0.14 nM
|
|
|
|
98.76% |
AG-494 |
|
|
|
|
99.31% |
PD-161570 |
|
|
|
|
99.82% |
EGFR/ErbB-2/ErbB-4 inhibitor-2 |
|
|
|
|
99.45% |
MS9449 |
EGFR (WT), Kd: 17 nM
EGFR L858R, Kd: 10 nM
|
|
|
|
98.95% |
Piperonylic acid |
|
|
|
|
99.91% |
EGFR-IN-12 |
EGFR (WT), IC50: 21 nM
EGFRL858R, IC50: 63 nM
EGFRL861Q, IC50: 4 nM
|
|
|
|
99.40% |
Anbenitamab |
|
|
|
|
99.22% |
GW2974 |
EGFRL858R/T790M, IC50: 0.007 μM
|
|
|
|
99.54% |
Selatinib |
|
|
|
|
99.83% |
PROTAC EGFR degrader 2 |
|
|
|
|
|
WHI-P180 |
|
|
|
|
99.62% |
AV-412 free base |
EGFR, IC50: 0.75 nM
EGFRL858R, IC50: 0.51 nM
EGFRL858R/T790M, IC50: 2.3 nM
EGFRT790M, IC50: 0.79 nM
|
|
|
|
98.33% |
Theliatinib |
EGFR, IC50: 3 nM
EGFR, Ki: 0.05 nM
EGFR (L858R/T790M), IC50: 22 nM
|
|
|
|
99.77% |
TAS0728 |
|
|
|
|
99.15% |
EGFR-IN-11 |
EGFRL858R/T790M/C797S, IC50: 18 nM
|
|
|
|
99.30% |
Rociletinib hydrobromide |
EGFRL858R/T790M, Ki: 21.5 nM
EGFRT790M, Ki: 303.3 nM
|
|
|
|
98.04% |
Tyrphostin AG 528 |
|
|
|
|
≥98.0% |
PD-089828 |
EGFR, IC50: 5.47 μM
EGFR, Ki: 3.16 μM
|
|
|
|
98.07% |
RG14620 |
EGFR, IC50: 3 μM (Cell Assay)
|
|
|
|
98.09% |
Mutant EGFR inhibitor |
EGFRL858R
EGFRExon 19 deletion
EGFRT790M
|
|
|
|
99.51% |
CGP52411 |
|
|
|
|
99.82% |
CNX-2006 |
|
|
|
|
98.42% |
EGFR-IN-7 |
EGFR (WT), IC50: 7.92 nM
EGFR (C797S/T790M/L858R), IC50: 0.218 nM
|
|
|
|
99.76% |
Cinrebafusp alfa |
|
|
|
|
98.53% |
(E)-AG 99 |
|
|
|
|
98.36% |
EGFR-IN-5 |
EGFR, IC50: 10.4 nM
EGFRL858R, IC50: 1.1 nM
EGFRL858R/T790M, IC50: 34 nM
EGFRL858R/T790M/C797S, IC50: 7.2 nM
|
|
|
|
98.64% |
Lavendustin C |
|
|
|
|
98.32% |
EGFR-IN-89 |
EGFR19del/TM/CS, IC50: 10.1 nM
|
|
|
|
|
PROTAC EGFR degrader 9 |
EGFRL858R/T790M/C797S, DC50: 10.2 nM
EGFRL858R/T790M/C797S, Kd: 240.2 nM
EGFRdel19 T790M C797S, DC50: 36.5 nM
EGFRL858R/T790M, DC50: 88.5 nM
EGFRdel19, DC50: 75.4 nM
EGFR (WT), DC50: >300 nM
|
|
|
|
98.35% |
EMI1 |
EGFRdel19 T790M C797S
EGFRL858R/T790M/C797S
|
|
|
|
99.78% |
AG 555 |
|
|
|
|
≥98.0% |
Astragaloside VI |
|
|
|
|
99.95% |
PROTAC EGFR degrader 7 |
EGFRL858R/T790M, DC50: 13.2 nM
|
|
|
|
99.99% |
NRC-2694 |
|
|
|
|
99.45% |
EGFR kinase inhibitor 3 |
EGFR (WT), IC50: <10 nM
EGFR L858R, IC50: 1.5 nM
EGFR L858R/T790M, IC50: 0.059 nM
EGFR L858R/T790M/C797S, IC50: 0.064 nM
|
|
|
|
|
EGFR/HER2-IN-9 |
EGFR, IC50: 3.2 nM
EGFRT790M, IC50: 8.3 nM
|
|
|
|
98.73% |
JNJ28871063 hydrochloride |
|
|
|
|
98.36% |
AV-412 |
EGFR, IC50: 0.75 nM
EGFRL858R, IC50: 0.5 nM
EGFRT790M, IC50: 0.79 nM
EGFRL858R/T790M, IC50: 2.3 nM
|
|
|
|
99.17% |
ZD-4190 |
|
|
|
|
98.08% |
Firmonertinib |
|
|
|
|
99.89% |
Epertinib |
EGFR, IC50: 1.48 ± 0.0 nM
|
HER2, IC50: 7.15 ± 0.5 nM
|
|
HER4, IC50: 2.49 ± 0.1 nM
|
≥98.0% |
EGFR-IN-1 hydrochloride |
|
|
|
|
|
MC-Val-Cit-PAB-Amide-TLR7 agonist 4 |
|
|
|
|
99.39% |
Mutated EGFR-IN-3 |
EGFRL858R/T790M, IC50: 12 nM
EGFRC797S, IC50: 13 nM
|
|
|
|
|
JBJ-09-063 |
EGFR L858R, IC50: 0.147 nM
EGFR L858R/T790M, IC50: 0.063 nM
EGFR L858R/T790M/C797S, IC50: 0.083 nM
EGFRLT/L747S, IC50: 0.396 nM
|
|
|
|
|
DBPR112 |
EGFRL858R/T790M, IC50: 48 nM
EGFRWT, IC50: 15 nM
|
|
|
|
98.37% |
MS9427 |
EGFR (WT), Kd: 7.1 nM
EGFR L858R, Kd: 4.3 nM
|
|
|
|
|
Larotinib |
EGFR (WT), IC50: 0.611 nM
EGFRL858R, IC50: 0.563 nM
EGFRL861Q, IC50: 0.423 nM
EGFRT790M, IC50: 45.2 nM
|
|
|
|
99.50% |
(S)-Sunvozertinib |
EGFR exon 20 NPH, IC50: 51.2 nM
EGFR exon 20 ASV insertion, IC50: 51.9 nM
EGFRL858R/T790M, IC50: 1 nM
|
Her2 exon 20 YVMA insertion, IC50: 21.2 nM
|
|
|
99.14% |
EGFR-IN-1 |
|
|
|
|
|
EGFR-IN-17 |
EGFR (C797S/T790M/L858R), IC50: 0.0002 μM
|
|
|
|
98.42% |
JBJ-04-125-02 |
EGFR (L858R/T790M), IC50: 0.26 nM
|
|
|
|
|
YS-363 |
|
|
|
|
99.52% |
HX103 |
EGFRdel19, IC50: 1.3 nM
EGFRL858R, IC50: 1.5 nM
EGFRT790M, IC50: 977 nM
EGFRWT, IC50: 4.0 nM
|
|
|
|
99.10% |
EGFR-IN-69 |
EGFR L858R/T790M/C797S, IC50: 4.3 ± 0.9 nM
EGFRL858R/T790M, IC50: 6.6 ± 0.8 nM
EGFRdel19 T790M C797S, IC50: 25.6 ± 7.5 nM
EGFRWT, IC50: 816.0 ± 82 nM
|
|
|
|
99.58% |
SU5204 |
|
|
|
|
99.46% |
pan-HER-IN-2 |
EGFR, IC50: 0.72 nM
EGFR (L858R/T790M), IC50: 8.2 nM
|
|
|
|
98.10% |
EGFR-IN-1 TFA |
|
|
|
|
99.38% |
Inetetamab |
|
|
|
|
|
T-1-PMPA |
EGFRWT, IC50: 86 nM
EGFRT790M, IC50: 561.73 nM
|
|
|
|
99.70% |
ZM 449829 |
|
|
|
|
99.73% |
Nazartinib mesylate |
EGFRL858R/T790M, Ki: 31 nM
|
|
|
|
|
BGB-102 |
|
|
|
|
99.52% |
Allitinib |
EGFR, IC50: 0.5 nM
EGFRL858R/T790M, IC50: 12 nM
|
|
|
|
99.36% |
Afatinib oxalate |
EGFRL858R, IC50: 0.4 nM
EGFRWT, IC50: 0.5 nM
EGFRL858R/T790M, IC50: 10 nM
|
|
|
|
|
Mobocertinib mesylate |
EGFR exon 20 insertion
EGFR (WT)
|
|
|
|
|
Lapatinib tosylate |
|
|
|
|
|
JBJ-02-112-05 |
EGFRL858R/T790M, IC50: 15 nM
|
|
|
|
|
ZN-A-1041 |
|
|
|
|
|
Mutated EGFR-IN-2 |
EGFR (L858R/T790M), IC50: <1 nM
|
|
|
|
|
TX2-121-1 |
|
|
|
|
|
EGFR/CSC-IN-1 |
|
|
|
|
|
EMI56 |
EGFRL858R/T790M/C797S
EGFRdel19 T790M C797S
|
|
|
|
99.72% |
EGFR/HER2-IN-2 |
|
|
|
|
|
SU 5402 (GMP) |
|
|
|
|
|
Gancotamab |
|
|
|
|
|
Oritinib mesylate |
EGFR (WT), IC50: 18 nM
EGFRL858R, IC50: 0.7 nM
EGFRL861Q, IC50: 4 nM
EGFRL858R/T790M, IC50: 0.1 nM
EGFRd746-750, IC50: 1.4 nM
EGFRd746-750/T790M, IC50: 0.89 nM
|
|
|
|
|
Sacibertinib |
EGFR-TK phosphorylation, EC50: 110 nM
|
|
|
|
|
EMI48 |
EGFRL858R/T790M/C797S
EGFRdel19 T790M C797S
|
|
|
|
99.02% |
EGFR-IN-15 |
|
|
|
|
|
EGFR-IN-29 |
|
|
|
|
|
HER2-IN-20 |
|
HER2(WT), IC50: 49 nM
HER2 YVMA, IC50: 42 nM
|
|
|
|
Nelipepimut-S |
|
|
|
|
|
HER2-IN-14 |
|
|
|
|
|
DPPY |
|
|
|
|
|
EGFR kinase inhibitor 1 |
EGFR (WT), IC50: 37 nM
EGFRL858R/T790M, IC50: 1.7 nM
EGFRL858R/T790M/C797S, IC50: >300 nM
|
|
|
|
|
EGFR/HER2-IN-10 |
|
|
|
|
|
GLUT1/EGFR-IN-1 |
|
|
|
|
|
EGFR-IN-75 |
EGFRWT, IC50: 0.28 μM
EGFRT790M, IC50: 5.02 μM
|
|
|
|
|
EGFR/HER2/TS-IN-2 |
EGFR, IC50: 0.173 ± 0. μM
|
HER2, IC50: 0.125 ± 0. μM
|
|
|
|
EGFR T790M/L858R-IN-2 |
EGFRL858R/T790M, IC50: 3.5 nM
EGFR (WT), IC50: 1290 nM
EGFRT790M, IC50: 6.7 nM
EGFRL858R, IC50: 2.1 nM
|
|
|
|
99.66% |
HER2-IN-9 |
|
|
|
|
|
EGFR/VEGFR2-IN-3 |
|
|
|
|
|
EGFR-IN-80 |
|
|
|
|
|
2′-Thioadenosine |
|
|
|
|
|
EGFR WT/T790M-IN-2 |
EGFRT790M, IC50: 0.08 μM
EGFRWT, IC50: 0.13 μM
|
|
|
|
|
EGFR-IN-116 |
|
|
|
|
|
EGFR-IN-54 |
|
|
|
|
|
BMS-599626 dihydrochloride |
|
|
|
|
|
EGFR-IN-73 |
EGFRdel19, IC50: 119 nM
EGFRL858R, IC50: 820 nM
EGFRWT, IC50: >10 μM
EGFRL858R/T790M, IC50: >10 μM
|
|
|
|
|
EGFR-IN-51 |
EGFR, IC50: 0.493 μM
EGFRL858R, IC50: 102.60 μM
EGFRT790M, IC50: 461.63 μM
|
|
|
|
|
EGFR-IN-3 |
|
|
|
|
|
HER2-IN-5 |
|
|
|
|
|
PDE5-IN-3 |
|
|
|
|
|
EGFR-IN-28 |
|
|
|
|
|
EGFR-IN-120 |
EGFRL858R/T790M/C797S, IC50: 0.053 μM
|
|
|
|
|
JGK-068S |
|
|
|
|
|
EGFR-IN-127 |
EGFRex19del, IC50: 136.3 nM
EGFR19del/TM/CS, IC50: 161.2 nM
|
|
|
|
|
EGFR-IN-60 |
EGFR, IC50: 0.083 μM
EGFRL858R, IC50: 0.053 μM
EGFRT790M, IC50: 0.026 μM
|
|
|
|
|
Tyrphostin 8 |
|
|
|
|
≥98.0% |
pan-HER-IN-1 |
EGFR, IC50: 0.38 nM
EGFRL858R/T790M/C797S, IC50: 2.2 nM
|
|
|
|
|
TAS-121 |
EGFR L858R, IC50: 1.7 nM
EGFR (ex19del), IC50: 2.7 nM
EGFR L858R/T790M, IC50: 0.56 nM
EGFR (ex19del/T790M), IC50: 1.1 nM
EGFR (WT), IC50: 8.2 nM
|
|
|
|
|
EGFR-IN-67 |
|
|
|
|
|
EGFR-IN-21 |
|
|
|
|
|
EGFR/HER2-IN-5 |
|
|
|
|
|
EGFR/HER2-IN-15 |
EGFR (WT), IC50: 37.21 nM
|
|
|
|
|
EGFR-IN-92 |
|
|
|
|
|
CHMFL-EGFR-202 |
EGFRT790M, IC50: 5.3 nM
EGFR, IC50: 8.3 nM
|
|
|
|
99.75% |
EGFR T790M/L858R-IN-6 |
|
|
|
|
|
EGFR-IN-49 |
EGFRT790M, IC50: 65.0 nM
EGFRL858R/T790M, IC50: 13.6 nM
|
|
|
|
|
EGFR-IN-74 |
EGFRL858R/T790M, IC50: 138 nM
|
|
|
|
|
HER2-IN-15 |
|
Her2 exon 20 YVMA insertion, IC50: <200 nM
|
|
|
|
Chrysophanol (Standard) |
|
|
|
|
|
MJ04 |
|
|
|
|
|
EGFR/HER2-IN-4 |
|
|
|
|
|
EGFR-IN-131 |
|
|
|
|
|
EGFR-IN-124 |
|
|
|
|
|
EGFR-IN-16 |
|
|
|
|
|
EGFR-IN-104 |
EGFRL858R/T790M, IC50: 0.33 μM
EGFRL858R/T790M/C797S, IC50: 0.133 μM
|
|
|
|
|
AG-1478 hydrochloride |
|
|
|
|
|
Gamendazole |
|
|
|
|
|
EGFR/HER2-IN-16 |
EGFR, IC50: 6.15 nM
HER1, IC50: 9.78 nM
|
|
|
|
|
EGFR-IN-40 |
|
|
|
|
|
EGFR kinase inhibitor 7 |
|
|
|
|
|
EGFR-IN-105 |
|
|
|
|
|
EGFR-IN-56 |
EGFRT790M, IC50: 541.7 nM
EGFRL858R/T790M, IC50: 132.1 nM
|
|
|
|
|
HER2-IN-8 |
|
|
|
|
|
EGFR-IN-132 |
|
|
|
|
|
HER2-IN-17 |
|
Her2 exon 20 YVMA insertion, IC50: <200 nM
|
|
|
|
PROTAC EGFR degrader 5 |
|
|
|
|
|
Multi-kinase-IN-4 |
|
|
|
|
|
HER2-IN-13 |
|
|
|
|
|
EGFR-IN-27 |
EGFRdel19, IC50: <50 nM
EGFRL858R, IC50: <50 nM
EGFRL858R/T790M, IC50: <50 nM
EGFRdel19 T790M C797S, IC50: <50 nM
EGFR (C797S/T790M/L858R), IC50: <50 nM
EGFRdel19 T790M, IC50: <50 nM
|
|
|
|
|
EGFR-IN-64 |
|
|
|
|
|
EGFR-IN-45 |
|
|
|
|
|
HSP90-IN-13 |
|
|
|
|
|
EGFR-IN-106 |
|
|
|
|
|
RET-IN-19 |
EGFR, IC50: 56.78 ± 4. μM
|
|
|
|
|
EP26 |
|
|
|
|
|
EGFR-IN-109 |
EGFR, IC50: 25.8 nM
EGFRT790M, IC50: 182.3 nM
|
|
|
|
|
HER2-IN-18 |
EGFR (WT), IC50: 500-1500 n nM
|
HER2(WT), IC50: <200 nM
HER2 YVMA, IC50: <200 nM
|
|
|
|
EGFR-IN-9 |
EGFR (WT), IC50: 7 nM
EGFRL858R/T790M, IC50: 28 nM
|
|
|
|
98.84% |
EGFR/HER2/TS-IN-1 |
|
|
|
|
|
EGFR/BRAF-IN-1 |
|
|
|
|
|
EGFR-IN-30 |
EGFR (WT), IC50: 1-10 nM
EGFR (L858R/T790M/C797S), IC50: <1 nM
|
|
|
|
|
Multi-kinase-IN-6 |
|
|
|
|
|
EGFR-IN-133 |
|
|
|
|
|
EGFR T790M/L858R-IN-4 |
|
|
|
|
|
EGFR-IN-46 |
|
|
|
|
|
EGFR-IN-61 |
EGFRL858R/T790M, IC50: 42 ± 2 nM
EGFRL858R/T790M/C797S, IC50: 137 ± 6 nM
EGFR (WT), IC50: 743 ± 20 nM
|
|
|
|
|
EGFR-IN-53 |
|
|
|
|
|
EGFR-IN-134 |
|
|
|
|
|
EGFR-IN-52 |
EGFR, IC50: 0.358 μM
EGFRL858R, IC50: 86.02 μM
EGFRT790M, IC50: 432.67 μM
|
|
|
|
|
HER2-IN-16 |
|
Her2 exon 20 YVMA insertion, IC50: <200 nM
|
|
|
|
EGFR-IN-55 |
EGFRL858R/T790M, IC50: 3.9 nM
EGFRWT, IC50: 70 nM
|
|
|
|
|
EGFR-IN-115 |
|
|
|
|
|
EGFR/C797S-IN-1 |
EGFRL858R/T790M/C797S, IC50: 0.128 μM
|
|
|
|
|
EGFR ligand-2 |
EGFRL858R, IC50: 21 nM
EGFRL858R/T790M, IC50: 48 nM
|
|
|
|
|
EGFR/HER2/DHFR-IN-3 |
|
|
|
|
|
PD 173955 analog 1 |
|
|
|
|
|
Simotinib hydrochloride |
|
|
|
|
|
HER2-IN-12 |
|
|
|
|
|
EGFR-IN-57 |
|
|
|
|
|
EGFR/HER2-IN-3 |
|
|
|
|
|
(E/Z)-CP-724714 |
|
|
|
|
|
EGFR-IN-62 |
EGFRL858R/T790M, IC50: 10 ± 1
EGFR (WT), IC50: 29 ± 2
EGFRL858R/T790M/C797S, IC50: 242 ± 9
|
|
|
|
|
EGFR-IN-36 |
EGFR (WT), IC50: 19.09 nM
|
HER2(WT), IC50: 120.01 nM
HER2 (A775_G776insYVMA), IC50: 2.35 nM
|
|
|
|
EGFR-IN-22 |
EGFRL858R/T790M/C797S, IC50: 0.54 nM
EGFR (WT), IC50: 4.91 nM
|
|
|
|
|
D-69491 hydrochloride |
|
|
|
|
|
WHI-P180 hydrochloride |
|
|
|
|
|
SHR-A1201 |
|
|
|
|
|
SU-4313 |
|
|
|
|
|
Neptinib |
EGFR (WT), IC50: 0.24 nM
EGFRL858R/T790M, IC50: 7.25 nM
EGFRL858R, IC50: 0.46 nM
EGFRT790M, IC50: 1.79 nM
|
|
|
|
|
Herceptide |
|
|
|
|
|
Trastuzumab rezetecan |
|
|
|
|
|
GW837016X |
|
|
|
|
|
Calotatug ginistinag |
|
|
|
|
|
Erlotinib mesylate |
|
|
|
|
|