2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR MAPK/ERK Pathway Stem Cell/Wnt
  3. EGFR Akt ERK Ribosomal S6 Kinase (RSK)
  4. BI-4732

BI-4732 is an orally bioavailable, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC).

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

BI-4732 Chemical Structure

BI-4732 Chemical Structure

CAS No. : 2769715-68-4

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Based on 1 publication(s) in Google Scholar

BI-4732 Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

View All Akt Isoform Specific Products:

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Akt Akt1 Akt2 Akt3

View All ERK Isoform Specific Products:

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ERK ERK1 ERK2 ERK5 ERK8

View All Ribosomal S6 Kinase (RSK) Isoform Specific Products:

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p70S6K RSK2 RSK3 RSK4

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Description

BI-4732 is an orally bioavailable, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC)[1].

In Vitro

BI-4732(1-1000 nM, 72 h) exhibits potent anti-proliferative activity against EGFR_E19del/C797S (IC50 = 6 nM), EGFR_L858R/C797S (IC50 = 213 nM), EGFR_E19del/T790M/C797S (IC50 = 4 nM), and EGFR_L858R/T790M/C797S (IC50 = 15 nM) in Ba/F3 cells[1].
BI-4732(10-100 nM, 6 h) inhibits EGFR and downstream signaling phosphorylation in all EGFR_C797S Ba/F3 cells when combined with Osimertinib (HY-15772)[1].
BI-4732 (1-1000 nM, 72 h) shows potent antiproliferative activity against YU-1182, YU-1097, YUO-143, PC9, and PC9_DC cells, with [1].
values of 73 nM, 3 nM, 5 nM, 14 nM, and 25 nM, respectively[1].
BI-4732 (1-30 nM, 21 days) almost completely prevents clonogenicity in YUX-1024, PC9_DC, YU-1182 and YU-1097 cells when combined with Osimertinib (HY-15772)[1].

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

BI-4732 Related Antibodies

Western Blot Analysis[1]

Cell Line: All EGFR_C797S Ba/F3 cells
Concentration: 10, 100 nM combined with Osimertinib
Incubation Time: 6 h
Result: Reduced the phosphorylation of AKT, ERK, and S6K.
In Vivo

BI-4732 (2.5-25 mg/kg, p.o., twice daily, 4 weeks) demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S when used alone or combined with Osimertinib[1].

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

Animal Model: YU-1097 cells (5 × 106 in 100 µL PBS) were subcutaneously implanted into the flanks of 6-week-old female BALB/c nude mice[1]
Dosage: 2.5, 5, 10, 25 mg/kg or 5 mg/kg combined with Osimertinib (25 mg/kg)
Administration: p.o. twice daily for 4 weeks
Result: Achieved tumor growth inhibition (TGI) rates of 143.1%, 154.0%, 174.1%, and 183.2% at doses of 2.5, 5, 10, and 25 mg/kg, respectively.
Showed no significant changes in body weight.
Reduced the Ki67 expression.
Appeared phosphorylation of EGFR and its downstream molecules, AKT, ERK, and S6K after 6 h.
Showed greater tumor regression with 176.2% TGI when combined with Osimertinib.
Molecular Weight

592.69

Formula

C32H36N10O2
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(C=NN2C3=NC(N4C[C@@H]5OC[C@H]4C5)=C6C(N(C)C(N7C[C@@H](CCC8)N8CC7)=N6)=C3)C2=CC(C9=C(OC)C=CN=C9)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (3.37 mM; ultrasonic and warming and heat to 60°C; 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 1.6872 mL 8.4361 mL 16.8722 mL
5 mM --- --- ---
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 (protect from light). 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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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 (protect from light). 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 1.6872 mL 8.4361 mL 16.8722 mL 42.1806 mL
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BI-4732 Related Classifications

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  • 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:

BI-47322769715-68-4BI4732BI 4732EGFRAktERKRibosomal S6 Kinase (RSK)Epidermal growth factor receptorErbB-1HER1PKBProtein kinase BExtracellular signal regulated kinasesS6Kosimertinibantitumor blood-brain barrierInhibitorinhibitorinhibit

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