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

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.

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EGFR-IN-1 TFA Chemical Structure

EGFR-IN-1 TFA Chemical Structure

CAS No. : 2753348-63-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 539 In-stock
Solution
10 mM * 1 mL in DMSO USD 539 In-stock
Solid
5 mg USD 390 In-stock
10 mg USD 625 In-stock
25 mg USD 1250 In-stock
50 mg USD 2000 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of EGFR-IN-1 TFA:

EGFR-IN-1 TFA Related Antibodies

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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].

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

EGFR-IN-1 TFA Related Antibodies

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].

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

628.60

Formula

C30H31F3N6O6
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (397.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5908 mL 7.9542 mL 15.9084 mL 39.7709 mL
5 mM 0.3182 mL 1.5908 mL 3.1817 mL 7.9542 mL
10 mM 0.1591 mL 0.7954 mL 1.5908 mL 3.9771 mL
15 mM 0.1061 mL 0.5303 mL 1.0606 mL 2.6514 mL
20 mM 0.0795 mL 0.3977 mL 0.7954 mL 1.9885 mL
25 mM 0.0636 mL 0.3182 mL 0.6363 mL 1.5908 mL
30 mM 0.0530 mL 0.2651 mL 0.5303 mL 1.3257 mL
40 mM 0.0398 mL 0.1989 mL 0.3977 mL 0.9943 mL
50 mM 0.0318 mL 0.1591 mL 0.3182 mL 0.7954 mL
60 mM 0.0265 mL 0.1326 mL 0.2651 mL 0.6628 mL
80 mM 0.0199 mL 0.0994 mL 0.1989 mL 0.4971 mL
100 mM 0.0159 mL 0.0795 mL 0.1591 mL 0.3977 mL
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EGFR-IN-1 TFA Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR-IN-12753348-63-7EGFREpidermal growth factor receptorErbB-1HER1oralnonsmallcelllungcancerNSCLCH1975mutantHCC827phosphorylationInhibitorinhibitorinhibit

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