BGB-102

Alias: JNJ26483327; BGB102; JNJ 26483327; BGB-102; JNJ-26483327; BGB 102.
Cat No.:V4519 Purity: ≥98%
JNJ-26483327 (also known as BGB102; JNJ26483327; BGB-102) is a novel, potent, reversible and orally bioavailable small-molecule multitargeted tyrosine kinase inhibitor againstEGFR,HER2, andHER4withIC50s of 9.6 nM, 18 nM and 40.3 nM, respectively.
BGB-102 Chemical Structure CAS No.: 807640-87-5
Product category: New7
This product is for research use only, not for human use. We do not sell to patients.
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10mg
25mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

JNJ-26483327 (also known as BGB102; JNJ26483327; BGB-102) is a novel, potent, reversible and orally bioavailable small-molecule multitargeted tyrosine kinase inhibitor against EGFR, HER2, and HER4 with IC50s of 9.6 nM, 18 nM and 40.3 nM, respectively. It has potential antineoplastic activity. JNJ-26483327 binds to and inhibits several members of the epidermal growth factor receptor (EGFR) family, including EGFR, HER2 and HER4; Src family kinases (Lyn, Yes, Fyn, Lck and Src); and vascular endothelial growth factor receptor type 3 (VEGFR3).

Biological Activity I Assay Protocols (From Reference)
ln Vitro
When JNJ-26483327 (5 µM or 10 µM) and Herceptin are administered together, SKBR3 cells' HER2 phosphorylation is decreased. After 3, 6, or 8 days of therapy, JNJ-26483327 had a stronger inhibitory effect on cell viability compared to Herceptin or JNJ-26483327 by itself. When compared to Herceptin alone and TAPI-1, JNJ-26483327 had a reduced inhibitory effect on cell survival in SKBR3 and BT474 cells [1].
ln Vivo
In comparison to vehicle treatment, JNJ-26483327 (75 mg/kg, oral) delayed the growth of xenograft tumors; but, when combined with Herceptin, they removed the PKB feedback loop and were more successful in reducing the growth of xenograft tumors. possess a synergistic impact[1].
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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H25BRN4O2
Molecular Weight
457.363504171371
CAS #
807640-87-5
SMILES
CN1CCCCCOC(C(OC)=C2)=CC3=C2N=CN=C3NC4=CC(Br)=CC=C4C1
InChi Key
JXDYOSVKVSQGJM-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H25BrN4O2/c1-27-8-4-3-5-9-29-21-11-17-19(12-20(21)28-2)24-14-25-22(17)26-18-10-16(23)7-6-15(18)13-27/h6-7,10-12,14H,3-5,8-9,13H2,1-2H3,(H,24,25,26)
Chemical Name
35-bromo-17-methoxy-5-methyl-11-oxa-2,5-diaza-1(4,6)-quinazolina-3(1,2)-benzenacycloundecaphane
Synonyms
JNJ26483327; BGB102; JNJ 26483327; BGB-102; JNJ-26483327; BGB 102.
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • BGB-102


    Herceptin induces the activation of HER receptors and their dimerisation with HER2 as a result of an up-regulation and the release of HER ligands.

  • BGB-102


    nhibiting PKB phosphorylation by a PKB inhibitor induces up-regulation of heregulin and ADAM17.2010 Dec 21;8(12):e1000563.

  • BGB-102


    Combination of Herceptin with ADAM inhibitors decreases HER2 phosphorylation and is additive in cell viability inhibition.2010 Dec 21;8(12):e1000563.

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