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Cat. No.: HY-100520

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EGFR-IN-2

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

For research use only. We do not sell to patients.

CAS No.: 1643497-70-4
Formula: C₂₆H₃₃N₉O₃S
Molecular Weight:551.66

Storage:

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

Data Sheet (276 KB)

EGFR-IN-2 Chemical Structure

CAS No.: 1643497-70-4

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Use of MCE Products

Antibody-Drug Conjugates

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Protocol
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

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

IC₅₀ & Target

EGFR^[1]

All EGFR Isoforms :

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

CAS No. 1643497-70-4
Molecular Weight 551.66
Formula 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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocol

Animal Administration^[1]

Mice^[1]
Eight week old female SCID beige mice are inoculated subcutaneously with 5×10⁶ NCI-H1975 cells. When tumors reach a mean volume of 300 to 500 mm³, mice with similarly sized tumors are randomized into treatment groups. EGFR-IN-2 at 50 mg/kg or 100 mg/kg is administered orally as a single dose. Tumor and plasma samples are collected at 2, 8 or 16 h post dose^[1].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Handling Instructions (2659 KB)

References

[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]

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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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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protocol
Purity & Documentation
References

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EGFR-IN-2

All EGFR Isoforms

Biological Activity

Chemical Information

Protocol

Purity & Documentation

References

Calculators

Help & FAQs

EGFR-IN-2 Related Classifications

HY-100520 Related Classifications