1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. EGFR-IN-1 TFA

EGFR-IN-1 TFA 

Cat. No.: HY-19617B
Handling Instructions

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

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

EGFR-IN-1 TFA Chemical Structure

EGFR-IN-1 TFA Chemical Structure

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5 mg USD 480 In-stock
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10 mg USD 800 In-stock
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25 mg USD 1700 In-stock
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50 mg USD 2800 In-stock
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100 mg USD 4300 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of EGFR-IN-1 TFA:

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Description

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

IC50 & Target[1]

EGFRL858R/T790M

 

In Vitro

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

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 TFA (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 TFA evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 TFA shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 TFA reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h[1].

Molecular Weight

628.60

Formula

C₃₀H₃₁F₃N₆O₆

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.OC(C(F)(F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (397.71 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5908 mL 7.9542 mL 15.9084 mL
5 mM 0.3182 mL 1.5908 mL 3.1817 mL
10 mM 0.1591 mL 0.7954 mL 1.5908 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

EGFR-IN-1EGFREpidermal growth factor receptorErbB-1HER1oralnonsmallcelllungcancerNSCLCH1975mutantHCC827phosphorylationInhibitorinhibitorinhibit

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Product Name:
EGFR-IN-1 TFA
Cat. No.:
HY-19617B
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