2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis PI3K/Akt/mTOR Cell Cycle/DNA Damage
  3. EGFR Apoptosis Akt PERK
  4. EGFR-IN-175

EGFR-IN-175 is an orally active and selective EGFRL858R/T790M/C797S inhibitor with an IC50 of 18.94 nM. EGFR-IN-175 can induce cell apoptosis and cause G1 phase arrest. EGFR-IN-175 can downregulate p-EGFR, p-AKT, and p-ERK expression. EGFR-IN-175 can be used for the research of cancer, such as lung cancer.

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

EGFR-IN-175

EGFR-IN-175 Chemical Structure

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EGFR-IN-175 Related Antibodies

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Description

EGFR-IN-175 is an orally active and selective EGFRL858R/T790M/C797S inhibitor with an IC50 of 18.94 nM. EGFR-IN-175 can induce cell apoptosis and cause G1 phase arrest. EGFR-IN-175 can downregulate p-EGFR, p-AKT, and p-ERK expression. EGFR-IN-175 can be used for the research of cancer, such as lung cancer[1].

IC50 & Target[1]

EGFRWT

125.9 nM (IC50)

EGFRLR/TM

76.88 nM (IC50)

EGFRLR/TM/CS

18.94 nM (IC50)

In Vitro

EGFR-IN-175 (Compound M49) inhibits proliferation of BaF3-EGFRL858R/T790M/C797S, A431 and H1975 cells with IC50 values of 0.77, 5.11 and 5.94 μM[1].
EGFR-IN-175 (0.1-2.5 μM) dose-dependently downregulates phosphorylation levels of p-EGFR, p-AKT, and p-ERK in BaF3-TM cells[1].
EGFR-IN-175 (0.1-2.5 μM, 48 h) induces apoptosis and G1 phase arrest in BaF3-TM cells[1].

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

EGFR-IN-175 Related Antibodies

Apoptosis Analysis[1]

Cell Line: BaF3-TM cells
Concentration: 0.1, 1 and 2.5 μM
Incubation Time: 48 h
Result: Increased apoptosis rate, reaching 69.68% at 2.5 μM.
Upregulated protein expression of Cleaved-PARP and Cleaved-Caspase-3.
In Vivo

EGFR-IN-175 (Compound M49) (30 mg/kg for i.p., 30-60 mg/kg for p.o., once a day for 14 days) inhibits tumor growth in BaF3-EGFRL858R/T790M/C797S xenograft BALB/c nude mice[1].

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

Animal Model: BaF3-EGFRL858R/T790M/C797S xenograft BALB/c nude mice models[1]
Dosage: 30 mg/kg for i.p., 30 and 60 mg/kg for p.o
Administration: Once a day for 14 days
Result: Reduced tumor volume.
Reduced Ki67 and increased TUNEL-positive cells in tumors.
Downregulated p-EGFR.
Had no significant body weight loss and no toxicity to major organs.
Molecular Weight

702.85

Formula

C33H38N10O4S2
SMILES

O=C1C(C2=CC=CS2)=NC3=CN=C(NC4=CC=C(N5CCC(N6CCN(C)CC6)CC5)C=C4)N=C3N1C7=CN(S(=O)(C8CC8)=O)N=C7OC
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EGFR-IN-175 Related Classifications

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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-175EGFRApoptosisAktPERKEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasep-EGFRp-AKTand p-ERKBaF3-TMLung cancerInhibitorinhibitorinhibit

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HY-178009
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