1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. BGB-102

BGB-102 (Synonyms: JNJ-26483327)

Cat. No.: HY-15732
Handling Instructions

BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.

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

BGB-102 Chemical Structure

BGB-102 Chemical Structure

CAS No. : 807640-87-5

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BGB-102 is a potent multi-kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.

IC50 & Target[1]

EGFR

9.6 nM (IC50)

HER2

18 nM (IC50)

HER4

40.3 nM (IC50)

In Vitro

JNJ-26483327 (5 µM or 10 µM) with Herceptin treatment decreases HER2 phosphorylation in SKBR3 cells. JNJ-26483327 exerts greater inhibition of cell viability after 3, 6, or 8 d of treatment compared to Herceptin or JNJ-26483327 alone. JNJ-26483327 with TAPI-1 exerts less cell viability inhibition than Herceptin alone in both SKBR3 and BT474 cells[1].

In Vivo

JNJ-26483327 (75 mg/kg, p.o.) delays xenograft tumour growth compared to vehicle treatment, but when combines with Herceptin, they can abrogate the PKB feedback loop and is synergistic in inhibition of xenograft tumour growth[1].

Clinical Trial
Molecular Weight

457.36

Formula

C₂₂H₂₅BrN₄O₂

CAS No.

807640-87-5

SMILES

CN1CCCCCOC(C(OC)=C2)=CC3=C2N=CN/C3=N\C4=CC(Br)=CC=C4C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Cell Assay
[1]

SKBR3 and BT474 cells are grown in 24-well plates after seeding approximately 20,000 cells per well. The cells are grown for at least 24 h before treatment with 40 µg/mL Herceptin, 5 µM JNJ-26483327, 10 µM TAPI-1, 10 µM ADAM17 inhibitor, or a combination of these drugs for different durations. For the exogenous ligand experiments, 100 ng/mL EGF, heregulin, or betacellulin is added to the cells in addition to Herceptin (40 µg/mL) for a total of 5 d in BT474 cells. On the day of the experiment, the cells are trypsinized and diluted with PBS. The viable cells are counted using a cell counter.

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

Animal Administration
[1]

Human BT474 breast tumour cells are injected directly into the inguinal region of the male NMRI Nude mice (1×107 cells/200 mL/animal) on day 0. On day 25, when the tumour volume has reached an approximate average of 200 mm3, mice are randomized according to tumour volume, with ten mice per treatment group. Mice are then treated twice daily with either vehicle (30% Captisol) or vehicle containing JNJ-26483327 (75 mg/kg twice daily) by gavage (p.o.) for 21 d. Alternatively, mice are treated twice weekly with either vehicle (0.9% [w/v] NaCl) or a vehicle containing Herceptin (10 mg/kg) by intraperitoneal injection administered in a volume of 10 mL/kg body weight, for three cycles (i.e., 21 d). Another group receives combined doses of both agents. Tumour size and body weights are measured twice weekly, with mice monitored daily for clinical signs of toxicity for the duration of the treatment. Clinical signs of toxicity included (but are not limited to) persistent anorexia or dehydration, morbidity, lethargy, hypothermia, and/or laboured respiration.

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

BGB-102JNJ-26483327BGB102BGB 102JNJ26483327JNJ 26483327EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
BGB-102
Cat. No.:
HY-15732
Quantity:
MCE Japan Authorized Agent: