EGFR-IN-91
EGFR-IN-91 (compound 9) is an orally available EGFR inhibitor with blood-brain barrier penetrability. EGFR-IN-91 inhibits EGFRL858R/C797S and EGFRexon 19del/C797S, inducing tumor regression in xenograft (PDX) mouse models. EGFR-IN-91 has the potential to inhibit localized and metastatic non-small cell lung cancer (NSCLC) driven by EGFR mutants.
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- CAS No.: 3032113-20-2
- 화학식: C22H25ClFN5O3
- 분자량:461.92
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
83 nM
Compound: 9
|
Antiproliferative activity against human A-431 cells overexpressing wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human A-431 cells overexpressing wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 37934858] |
| AU565 | IC50 |
986 nM
Compound: 9
|
Antiproliferative activity against patient-derived HER2-positive human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against patient-derived HER2-positive human AU565 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 37934858] |
| HCC827 | IC50 |
3.1 nM
Compound: 9
|
Antiproliferative activity against human HCC827 cells harboring EGFR del E746_A750 mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human HCC827 cells harboring EGFR del E746_A750 mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 37934858] |
| NCI-H1975 | IC50 |
>10000 nM
Compound: 9
|
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 37934858] |
| NCI-H3255 | IC50 |
7.2 nM
Compound: 9
|
Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against human NCI-H3255 cells harboring EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 37934858] |
| SK-BR-3 | IC50 |
1510 nM
Compound: 9
|
Antiproliferative activity against patient-derived HER2-positive human SK-BR-3 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against patient-derived HER2-positive human SK-BR-3 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 37934858] |
| ZR-75-30 | IC50 |
1632 nM
Compound: 9
|
Antiproliferative activity against patient-derived HER2-positive human ZR-75-30 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
Antiproliferative activity against patient-derived HER2-positive human ZR-75-30 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay
|
[PMID: 37934858] |
Chemical Information
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CAS No. 3032113-20-2
-
분자량 461.92
-
화학식 C22H25ClFN5O3
-
SMILES
CN1CCN(OCCOC2=C(OC)C=C3N=CN=C(NC4=CC=CC(Cl)=C4F)C3=C2)CC1
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선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)