country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

Referencia número: HY-100520

Copy Link Print Information

EGFR-IN-2

Name: EGFR-IN-2
Brand: MedChemExpress
SKU: HY-100520
Price: 544.00 USD
Availability: InStock
Rating: 5 (1 reviews)

EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS: 1643497-70-4
Fòrmula: C₂₆H₃₃N₉O₃S
Peso molecular:551.66

Almacenamiento:

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

Data Sheet (276 KB)

EGFR-IN-2 Chemical Structure

No. CAS: 1643497-70-4

Tamaño

Precio

Stock

Cantidad

Amount: USD 0.00

* Seleccione Cantidad antes de agregar artículos.

Top Publications Citing

Use of MCE Products

Antibody-Drug Conjugates

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

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

EGFR-IN-2 is a a noncovalent, irreversible, mutant-selective second generation EGFR inhibitor.

IC₅₀ & Target

EGFR^[1]

Ver todos los productos específicos de isoformas EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H1975	IC₅₀	0.361 μM Compound: 21	Antiproliferative activity against human NCI-H1975 cells harboring harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability Antiproliferative activity against human NCI-H1975 cells harboring harboring EGFR L858R/T790M double mutant assessed as reduction in cell viability	[PMID: 27564586]
PC-9	IC₅₀	0.151 μM Compound: 21	Antiproliferative activity against human PC-9 cells harboring harboring EGFR del (746 to 750) mutant assessed as reduction in cell viability Antiproliferative activity against human PC-9 cells harboring harboring EGFR del (746 to 750) mutant assessed as reduction in cell viability	[PMID: 27564586]

In Vitro

EGFR-IN-2 (Compound 21) inhibits EGFR autophosphorylation with IC₅₀s of 0.027 μM, 0.009 μM ,0.033 μM , and 0.218 μM in double mutant TMLR cell line H1975, double mutant TMdel cell line PC9-ER, activating mutant del cell line PC9, and wild type cell line H292. In addition, EGFR-IN-2 demonstrats strong antiproliferative effect on the T790M mutant carrying H1975 cell line (IC₅₀=0.361 μM) and the single activating mutant PC9 cell line (IC₅₀=0.151 μM). Furthermore, EGFR-IN-2 also shows good selectivity against other kinases when evaluated in a 225-kinase panel (12/225 kinases inhibited at >70% when tested at 0.1 μM, 61-fold over the TMLR K_i and 63-fold over the TMdel K_i)^[1].

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

In Vivo

To examine its inhibitory effect on pEGFR levels in vivo, EGFR-IN-2 (Compound 21) is studied in a mouse H1975 (TMLR) xenograft model. After a single oral dose of 21 at 50 mg/kg, free plasma concentrations of EGFR-IN-2 at or exceeding the in vitro p-EGFR IC₅₀ of 0.027 μM are sustained over 8 h. When administered at 100 mg/kg, the coverage of p-EGFR IC₅₀ is extended to the last measured time point of 16 h postdose. Corresponding knockdown of p-EGFR and the downstream effectors pERK1/2 and AKT levels are observed at those time points, suggesting target engagement in vivo. In mouse, after intravenous and oral administration, the plasma clearance of EGFR-IN-2 is determined to be 104 mL/kg per min with a bioavailability of 19%. In dogs, the plasma clearance is 13 mL/kg per min with an oral bioavailability of 30%^[1].

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

Chemical Information

No. CAS 1643497-70-4
Peso molecular 551.66
Fòrmula C₂₆H₃₃N₉O₃S
SMILES

O=S(N(N=C1)C=C1C2=NC=CC(NC3=NC=C(C(N4CC(C(C)(O)C)C4)=NN5[C@H](CC)C)C5=C3)=N2)(C6CC6)=O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Chan BK, et al. Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor. J Med Chem. 2016 Oct 13;59(19):9080-9093. [Content Brief]

Calculators

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

Obtener un presupuesto En stock

Other size

Obtener un presupuesto