2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. SH-1092

SH-1092 is an orally active EGFR inhibitor with an IC50 of 0.96 nM against EGFRT790M/L858R and an IC50 of 6.1 nM against wild-type EGFR. SH-1092 exhibits anticancer activity against non-small cell lung cancer. SH-1092 can be used in studies related to non-small cell lung cancer.

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

SH-1092

SH-1092 Chemical Structure

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SH-1092 Related Antibodies

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Description

SH-1092 is an orally active EGFR inhibitor with an IC50 of 0.96 nM against EGFRT790M/L858R and an IC50 of 6.1 nM against wild-type EGFR. SH-1092 exhibits anticancer activity against non-small cell lung cancer. SH-1092 can be used in studies related to non-small cell lung cancer[1].

IC50 & Target[1]

EGFRL858R/T790M

0.96 nM (IC50)

EGFR (WT)

EGFR nM (IC50)

In Vitro

SH-1092 potently inhibits EGFRT790M/L858R with an IC50 of 0.96 nM; it also inhibits wild-type EGFR with an IC50 of 6.1 nM, exhibits moderate selectivity for the mutant form, and shows weak inhibitory effects on IGF1R and INSR[1].
SH-1092 (0.1 nM-10 μM; 72 h) inhibits the proliferation of H1975 (EGFRT790M/L858R) cells and A431 (wild-type EGFR) cells[1].

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

SH-1092 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: H1975 (EGFR T790M/L858R mutant) non-small cell lung cancer cell line, A431 (EGFR wild-type) non-small cell lung cancer cell line
Concentration: 0.1 nM-10 μM
Incubation Time: 72 h
Result: Inhibited the growth of H1975 cells with an IC50 of 8 nM.
Inhibited the growth of A431 cells with an IC50 of 362 nM.
Parmacokinetics
Species Dose Route T1/2 AUC0-t AUC0-∞ CL Tmax F
Mice[1] 1.25 mg/mL p.o. 2.7 h 1062 ng·h/mL 1092.9 ng·h/mL / 0.8 h 19.8 %
Mice[1] 0.2 mg/mL i.v. 0.5 h 429.1 ng·h/mL 429.4 ng·h/mL 4.9 L/h/kg / /
In Vivo

SH-1092 (25-50 mg/kg; p.o.; daily; 14 days) exhibits dose-dependent, significant antitumor activity against EGFR wild-type A431 NSCLC xenografts in female BALB/c nude mice with low acute toxicity[1].
SH-1092 (10-50 mg/kg; p.o.; daily; 14 days) exhibits dose-dependent, significant antitumor activity against EGFRT790M/L858R mutant H1975 NSCLC xenografts in female BALB/c nude mice with low acute toxicity[1].

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

Animal Model: BALB/c nude (female)[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: p.o.; daily; 14 days
Result: Significantly inhibited A431 xenograft tumor growth in a dose-dependent manner.
Did not change mouse body weight significantly during treatment, indicating low acute toxicity.
Animal Model: BALB/c nude (female)[1]
Dosage: 10 mg/kg; 25 mg/kg; 50 mg/kg
Administration: p.o.; daily; 14 days
Result: Significantly inhibited H1975 xenograft tumor growth in a dose-dependent manner.
Did not change mouse body weight significantly during treatment, indicating low acute toxicity.
Molecular Weight

541.64

Formula

C30H35N7O3
SMILES

C=CC(NC1=CC(NC2=NC=C(C)C(C3=CN4C5=C3C=CC=C5OCC4)=N2)=C(OC)C=C1N(CCN(C)C)C)=O
Shipping

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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SH-1092 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:

SH-1092SH1092SH 1092EGFREpidermal growth factor receptorErbB-1HER1CYP1A2INSRIGF1Rnon-small cell lung cancerA431 cellsEGFR (T790M/L858R)CYP3A4CYP2D6EGFR (wild-type)H1975 cellsInhibitorinhibitorinhibit

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