BGB-102 (Synonyms: JNJ-26483327)

Cat. No.: HY-15732 Purity: 99.52%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 807640-87-5

Size	Price	Stock	Quantity
1 mg	USD 398	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 990	In-stock	Estimated Time of Arrival: December 31
10 mg		Get quote
50 mg		Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All EGFR Isoform Specific Products:

View All Isoforms

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

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].

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

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].

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

Clinical Trial

Molecular Weight

457.36

Formula

C₂₂H₂₅BrN₄O₂

CAS No.

807640-87-5

Appearance

Solid

Color

White to off-white

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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

THF : ≥ 7.27 mg/mL (15.90 mM)

DMSO : 4.4 mg/mL (9.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1865 mL	10.9323 mL	21.8646 mL
5 mM	0.4373 mL	2.1865 mL	4.3729 mL
10 mM	0.2186 mL	1.0932 mL	2.1865 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.52%

Select Batch:

Data Sheet (280 KB) SDS (252 KB)

COA (258 KB) HNMR (391 KB) RP-HPLC (206 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Gijsen M, et al. HER2 phosphorylation is maintained by a PKB negative feedback loop in response to anti-HER2 herceptin in breast cancer. PLoS Biol. 2010 Dec 21;8(12):e1000563. [Content Brief]

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	[1]. Gijsen M, et al. HER2 phosphorylation is maintained by a PKB negative feedback loop in response to anti-HER2 herceptin in breast cancer. PLoS Biol. 2010 Dec 21;8(12):e1000563. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / THF	1 mM	2.1865 mL	10.9323 mL	21.8646 mL	54.6615 mL
DMSO / THF	5 mM	0.4373 mL	2.1865 mL	4.3729 mL	10.9323 mL
THF	10 mM	0.2186 mL	1.0932 mL	2.1865 mL	5.4662 mL
THF	15 mM	0.1458 mL	0.7288 mL	1.4576 mL	3.6441 mL

BGB-102 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:

BGB-102807640-87-5JNJ-26483327BGB102BGB 102JNJ26483327JNJ 26483327EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Salutation

Applicant Name *

Email Address *

Phone Number *

Organization Name *

Department *

Requested quantity *

Country or Region *

Remarks