1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
  2. EGFR

EGFR-IN-2 

Cat. No.: HY-100520
Handling Instructions

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

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

EGFR-IN-2 Chemical Structure

EGFR-IN-2 Chemical Structure

CAS No. : 1643497-70-4

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

EGFR[1]

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 Ki and 63-fold over the TMdel Ki)[1].

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8127 mL 9.0636 mL 18.1271 mL
5 mM 0.3625 mL 1.8127 mL 3.6254 mL
10 mM 0.1813 mL 0.9064 mL 1.8127 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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].

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

References
Molecular Weight

551.66

Formula

C₂₆H₃₃N₉O₃S

CAS No.

1643497-70-4

SMILES

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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
EGFR-IN-2
Cat. No.:
HY-100520
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EGFR-IN-2

Cat. No.: HY-100520