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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 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).
| 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].
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| 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].
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| 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
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| Additional Infomation |
Multitargeted Tyrosine Kinase Inhibitor JNJ-26483327 is an orally bioavailable, small-molecule, multitargeted reversible tyrosine kinase inhibitor with potential antineoplastic activity. Multitargeted tyrosine kinase inhibitor 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). By inhibiting several different signaling molecules that play crucial roles at various stages in tumorigenesis, this agent may inhibit tumor growth, invasion, migration and metastasis. In addition, JNJ-26483327 crosses the blood-brain barrier (BBB).
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| Molecular Formula |
C22H25BRN4O2
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|---|---|
| Molecular Weight |
457.363504171371
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| Exact Mass |
456.116
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| CAS # |
807640-87-5
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| Related CAS # |
807640-87-5;1021686-80-5 (2HBr salt);
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| PubChem CID |
11952856
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| Appearance |
White to off-white solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
29
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JXDYOSVKVSQGJM-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
35-bromo-17-methoxy-5-methyl-11-oxa-2,5-diaza-1(4,6)-quinazolina-3(1,2)-benzenacycloundecaphane
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| Synonyms |
JNJ26483327; BGB102; JNJ 26483327; BGB-102; JNJ-26483327; BGB 102.
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
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.
 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. |
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 nhibiting PKB phosphorylation by a PKB inhibitor induces up-regulation of heregulin and ADAM17.PLoS Biol.2010 Dec 21;8(12):e1000563. |
 Combination of Herceptin with ADAM inhibitors decreases HER2 phosphorylation and is additive in cell viability inhibition.PLoS Biol.2010 Dec 21;8(12):e1000563. |
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