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Art. -Nr.: HY-19617

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EGFR-IN-1

EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity.

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CAS. Nr.: 1625677-63-5
Formel: C₂₈H₃₀N₆O₄
Molecular Weight:514.58

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (275 KB)

EGFR-IN-1 Chemical Structure

CAS. Nr.: 1625677-63-5

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

EGFR^L858R/T790M

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	1054 nM Compound: 24	Inhibition of wild type EGFR phosphorylation in human A431 cells after 60 mins by mesoscale multiplex assay Inhibition of wild type EGFR phosphorylation in human A431 cells after 60 mins by mesoscale multiplex assay	[PMID: 26396685]
A-431	IC₅₀	2400 nM Compound: 24	Cytotoxicity against human A431 cells expressing wild-type EGFR assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay Cytotoxicity against human A431 cells expressing wild-type EGFR assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay	[PMID: 26396685]
HCC827	IC₅₀	28 nM Compound: 24	Cytotoxicity against human HCC827 cells harboring EGFR 746 to 750 deletion mutant assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay Cytotoxicity against human HCC827 cells harboring EGFR 746 to 750 deletion mutant assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay	[PMID: 26396685]
NCI-H1975	IC₅₀	4 nM Compound: 24	Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay	[PMID: 26396685]
NCI-H1975	IC₅₀	4 nM Compound: 24	Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 60 mins by mesoscale multiplex assay Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 60 mins by mesoscale multiplex assay	[PMID: 26396685]

In Vitro

EGFR-IN-1 (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively^[1].
EGFR-IN-1 inhibits p-EGFR in H1975 and HCC827 cells with IC₅₀s of 4 and 9 nM, respectively. EGFR-IN-1 highly selective against a panel of 100 kinases^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

NSCLC cell lines H1975 (T790M/L858R), HCC827 (∆746-750)
Concentration:

10 μM
Incubation Time:

72 hours
Result:

Inhibited H1975 nonsmall cell lung cancer cell line and the first line mutant HCC827 cell line with IC₅₀s of 4 and 28 nM, respectively.

In Vivo

EGFR-IN-1 (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight^[1].
EGFR-IN-1 evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female athymic nude mice (H1975 Tumor Xenograft)^[1]
Dosage:

30 mg/kg
Administration:

p.o.; daily for 2 weeks
Result:

Led to significant tumor growth inhibition with no observed loss in body weight.

Chemical Information

CAS. Nr. 1625677-63-5
Molecular Weight 514.58
Formel C₂₈H₃₀N₆O₄
SMILES

COC(C=C(OCCN(C)C)C=C1)=C1NC2=NC=C3C(N(C4=CC=CC(NC(C=C)=O)=C4)C(C=C3C)=O)=N2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wurz RP, et al. Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors. ACS Med Chem Lett. 2015 Jul 27;6(9):987-92. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
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EGFR-IN-1

Alle EGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

EGFR-IN-1 Related Classifications

HY-19617 Related Classifications