A Met inhibitor
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JNJ-26483327

Item No. 44468

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
17-bromo-1,8,9,10,11,12,13,14-octahydro-20-methoxy-13-methyl-4,6-ethenopyrimido[4,5-b][6,1,12]benzoxadiazacyclopentadecine
CAS Number
807640-87-5
Molecular Formula
C22H25BrN4O2
Formula Weight
457.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Methanol: Slightly soluble: 0.1-1 mg/ml
SMILES
BrC1=CC=C2C(NC3=C4C=C(OCCCCCN(C2)C)C(OC)=CC4=NC=N3)=C1
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)
InChi Key
JXDYOSVKVSQGJM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $155

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    5 mg

    $736

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    10 mg

    $1,240

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    Product Description

    JNJ-26483327 is an inhibitor of Met.1 It also inhibits EGFR, HER2, and HER4 (IC50s = 9.6, 18, and 40.3 nM, respectively). JNJ-26483327 (5 or 10 µM), in combination with trastuzumab, reduces HER2 phosphorylation in BT474 breast cancer cells. It decreases tumor volume when used in combination with trastuzumab in a BT474 mouse xenograft model when administered at a dose of 75 mg/kg twice per day.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gijsen, M., King, P., Perera, T., et al. HER2 phosphorylation is maintained by a PKB negative feedback loop in response to anti-HER2 herceptin in breast cancer. PLoS Biol. 8(12), e1000563 (2010).