About 29 results found for searched term "EGFR-IN-85" (0.127 seconds)
| Cat.No. | Name | Target |
|---|---|---|
| M42099 | EGFR-IN-85 | EGFR/HER2 |
| EGFR-IN-85 is an EGFR inhibitor. | ||
| M2424 | AZD9291 (Osimertinib) | EGFR/HER2 |
| Osimertinib; Mereletinib | ||
| Osimertinib (AZD-9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR, respectively. | ||
| M3569 | AST-1306 (TsOH) | EGFR/HER2 |
| AST-6; Allitinib tosylate | ||
| AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases, | ||
| M4977 | AZ5104 | FGFR |
| AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. | ||
| M5099 | Osimertinib mesylate (AZD-9291 mesylate) | EGFR/HER2 |
| Mereletinib Mesylate | ||
| Osimertinib mesylate (AZD-9291 mesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively. | ||
| M5164 | AZD3759 | EGFR/HER2 |
| Zorifertinib | ||
| AZD3759 (Zorifertinib) is a potent, oral active, CNS-penetrant EGFR inhibitor with IC50 of 0.3 nM, 0.2 nM, and 0.2 nM for EGFR (WT), EGFR (L858R), and EGFR (exon 19Del), respectively. | ||
| M5275 | Nazartinib | EGFR/HER2 |
| EGF816, NVS-816 | ||
| Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro. | ||
| M5307 | Afatinib dimaleate | EGFR/HER2 |
| BIBW 2992MA2; BIBW2992; Afatinib | ||
| Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. | ||
| M6081 | EAI045 | EGFR/HER2 |
| EAI045 is a fourth generation allosteric inhibitor of mutant EGFR, which inhibits EGFR at 10 μM ATP, EGFRL858R, EGFRT790M and EGFRL858R/T790M with IC50 values of 1.9, 0.019, 0.19 and 0.002 μM respectively. | ||
| M43838 | Almonertinib mesylate | EGFR/HER2 |
| HS-10296 mesylate | ||
| Almonertinib mesylate is an orally active, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR sensitization and T790M resistance mutations, and also shows strong inhibitory activity against T790M, T790M/L858R, and T790M/Del19, with IC50 of 0.37, 0.29, and 0.21 nM, respectively. The IC50 of T790M/Del19 was 0.37, 0.29 and 0.21 nM, respectively, but the inhibitory effect on wild-type was weaker, with an IC50 of 3.39 nM. It can be used in the research of non-small cell lung cancer. | ||
| M10475 | Lifirafenib (BGB-283) | Raf |
| Beigene-283 | ||
| Lifirafenib (BGB-283) is a novel potent and selective RAF Kinase and EGFR inhibitor with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant. | ||
| M11415 | (Rac)-JBJ-04-125-02 | EGFR/HER2 |
| JBJ-04-125-02 racemate | ||
| (Rac)-JBJ-04-125-02 is a racemate of JBJ-04-125-02, which is a potent, selectively mutated, allosteric and oral active EGFR inhibitor. The IC50 of EGFRL858R/T790M was 0.26 nM. | ||
| M11417 | (S)-Sunvozertinib | EGFR/HER2 |
| (S)-DZD9008 | ||
| (S)-Sunvozertinib ((S)-DZD9008) is the S-enantiomer of Sunvozertinib, EGFR exon 20 NPH and ASV insertion, EGFR L858R/T790M mutation and Her2 exon 20 YVMA insertion (IC50 was 51.2 nM, 51.9 nM, 1 nM and 21.2 nM, respectively). (S)-Sunvozertinib also inhibits BTK. | ||
| M11448 | BLU-945 | EGFR/HER2 |
| ZL-2313 | ||
| Blu-945 is a potent inhibitor of selective epidermal growth factor receptor (EGFR). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. | ||
| M14131 | AV-412 free base | EGFR/HER2 |
| MP-412 free base | ||
| AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. | ||
| M14132 | Osimertinib dimesylate | EGFR/HER2 |
| AZD-9291 dimesylate; Mereletinib dimesylate | ||
| Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively. | ||
| M14134 | Rociletinib hydrobromide | EGFR/HER2 |
| CO-1686 hydrobromide; AVL-301 hydrobromide; CNX-419 hydrobromide | ||
| Rociletinib hydrobromide (CO-1686 hydrobromide) is an orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M, and the Ki values for EGFRL858R/T790M and EGFRWT are 21.5 nM and 303.3 nM, respectively. | ||
| M14871 | Gefitinib-based PROTAC 3 | PROTAC |
| Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau 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, respectively. | ||
| M27980 | DBPR112 | EGFR/HER2 |
| DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor efficacy. | ||
| M29151 | JBJ-04-125-02 | EGFR/HER2 |
| JBJ-04-125-02 is a potent, mutant-selective, allosteric and orally active EGFR inhibitor with an IC50 of 0.26 nM for EGFRL858R/T790M. JBJ-04-125-02 can inhibit cancer cell proliferation and EGFRL858R/T790M/C797S signaling. JBJ-04-125-02 has anti-tumor activities. | ||
| M29464 | JND3229 | EGFR/HER2 |
| JND3229 is a reversible EGFRC797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFRL858R/T790M/C797S, EGFRWT and EGFRL858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma. | ||
| M29467 | EGFR-IN-7 | EGFR/HER2 |
| TQB3804 | ||
| EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers. | ||
| M29606 | NSC689857 | EGFR/HER2 |
| NSC689857 is a potent EGFR and SCFSKP2 inhibitor with an IC50 value of 36 μM for Skp2-Cks1. NSC689857 can inhibit p27 ubiquitylation (IC50=30 μM). NSC689857 has varied activity across cancer types, with more activity against leukemia cell lines than others. | ||
| M30826 | EAI001 | EGFR/HER2 |
| EAI001 is a potent, selective mutant epidermal growth factor receptor (EGFR) allosteric inhibitor with an IC50 value of 24 nM for EGFRL858R/T790M. EAI001 can be used for research of cancer. | ||
| M42074 | EGFR-IN-82 | EGFR/HER2 |
| EGFR-IN-82 is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively. | ||
| M42077 | EGFR T790M/L858R-IN-2 | EGFR/HER2 |
| EGFRT790M/L858R-IN-2 is a potent and selective EGFRT790M/L858R inhibitor with IC50 values of 3.5, 1290 nM for EGFRT790M/L858R, EGFR WT, respectively. | ||
| M56421 | EGFR-IN-5 | EGFR/HER2 |
| EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively. | ||
| M56420 | JBJ-09-063 | EGFR/HER2 |
| JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. | ||
| M56417 | EGFR-IN-16 | EGFR/HER2 |
| EGFR-IN-16 is a potent EGFR inhibitor with pIC50 of 4.85 and 4.74 for EGFR and HER-2, respectively. | ||
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