A dual PI3K and mTOR inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

NVP-BGT226

Item No. 22142

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1,3-dihydro-8-(6-methoxy-3-pyridinyl)-3-methyl-1-[4-(1-piperazinyl)-3-(trifluoromethyl)phenyl]-2H-imidazo[4,5-c]quinolin-2-one, (2Z)-2-butenedioate
CAS Number
1245537-68-1
Molecular Formula
C28H25F3N6O2 • C4H4O4
Formula Weight
650.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml
λmax
273 nm
SMILES
COC(N=C1)=CC=C1C2=CC3=C(C=C2)N=CC4=C3N(C5=CC=C(N6CCNCC6)C(C(F)(F)F)=C5)C(N4C)=O.OC(/C=C\C(O)=O)=O
InChi Code
InChI=1S/C28H25F3N6O2.C4H4O4/c1-35-24-16-33-22-6-3-17(18-4-8-25(39-2)34-15-18)13-20(22)26(24)37(27(35)38)19-5-7-23(21(14-19)28(29,30)31)36-11-9-32-10-12-36;5-3(6)1-2-4(7)8/h3-8,13-16,32H,9-12H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
InChi Key
YUXMAKUNSXIEKN-BTJKTKAUSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $44

    Add

    5 mg

    $161

    Add

    10 mg

    $302

    Add

    25 mg

    $696

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    NVP-BGT226 is an orally bioavailable dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR).1 It inhibits class I PI3Ks with EC50 values of 4, 63, and 38 nM for PI3Kα, β, and γ isoforms, respectively, in a filter binding assay. It binds to both class I and class III PI3Ks in a quantitative ELISA assay with EC50 values of 55.8 and 7.03 nM, for HsPI3Kβ and HsVps34, respectively.2 It decreases protein levels of phosphorylated mTOR and Akt, a downstream target of PI3K signaling.3 NVP-BGT226 inhibits the growth of squamous cell carcinoma cell lines, HONE-1, and a variant of HONE-1 resistant to cisplatin (Item No. 13119) with IC50 values of 7.4-27.8, 22.6, and 30.1 nM, respectively.4 It halts the cell cycle at the G0/G1 phase and induces autophagy. NVP-BGT226 (2.5 and 5 mg/kg daily for three weeks) inhibits tumor growth in a FaDu head and neck cancer mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Markman, B., Tabernero, J., Krop, I., et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann. Oncol. 23(9), 2399-2408 (2012).

    2. Hassett, M.R., Sternberg, A.R., and Roepe, P.D. Inhibition of human class I vs class III phosphatidylinositol 3'-kinases. Biochemistry 56(33), 4326-4334 (2017).

    3. Baumann, P., Schneider, L., Mandl-Weber, S., et al. Simultaneous targeting of PI3K and mTOR with NVP-BGT226 is highly effective in multiple myeloma. Anticancer Drugs 23(1), 131-138 (2012).

    4. Chang, K.-Y., Tsai, S.-Y., Wu, C.-M., et al. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin. Cancer Res. 17(22), 7116-7126 (2011).