Dual inhibitor of IGF-1R and InsR tyrosine kinases
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.

BMS 754807

Item No. 17505

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoro-3-pyridinyl)-2-methyl-(2S)-2-pyrrolidinecarboxamide
CAS Number
1001350-96-4
Molecular Formula
C23H24FN9O
Formula Weight
461.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
244, 312 nm
SMILES
FC1=NC=C(NC([C@]2(C)CCCN2C3=NN4C(C(NC5=NNC(C6CC6)=C5)=N3)=CC=C4)=O)C=C1
InChi Code
InChI=1S/C23H24FN9O/c1-23(21(34)26-15-7-8-18(24)25-13-15)9-3-10-32(23)22-28-20(17-4-2-11-33(17)31-22)27-19-12-16(29-30-19)14-5-6-14/h2,4,7-8,11-14H,3,5-6,9-10H2,1H3,(H,26,34)(H2,27,28,29,30,31)/t23-/m0/s1
InChi Key
LQVXSNNAFNGRAH-QHCPKHFHSA-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

    $49

    Add

    5 mg

    $223

    Add

    10 mg

    $354

    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

    BMS 754807 is a reversible, orally bioavailable dual inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases (IC50s = 1.8 and 1.7 nM, respectively).1,2 It has minimal effect against an array of other tyrosine and serine/threonine kinases.1 BMS 754807 inhibits cell proliferation or induces apoptosis in a variety of cancer cells in vitro.2 It inhibits the growth of tumor xenografts in mice and this effect is often enhanced by combination therapy with other chemotherapeutics.2,3,4 Predictive biomarkers, including elevated IGF-1R expression, for effectiveness of BMS 754807 have been delineated.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wittman, M.D., Carboni, J.M., Yang, Z., et al. Discovery of a 2,4-disubstituted pyrrolo-[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of insulin-like growth factor receptor (IGF-1R) kinase in clinical development. J. Med. Chem. 52(23), 7630-7363 (2009).

    2. Carboni, J.M., Wittman, M., Yang, Z., et al. BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR. Mol. Cancer Ther. 8(12), 3341-3349 (2009).

    3. Awasthi, N., Zhang, C., Ruan, W., et al. BMS-754807, a small-molecule inhibitor of insulin-like growth factor-1 receptor/insulin receptor, enhances gemcitabine response in pancreatic cancer. Mol. Cancer Ther. 11(12), 2644-2653 (2012).

    4. Dayyani, F., Parikh, N.U., Varkaris, A.S., et al. Combined inhibition of IGF-1R/IR and Src family kinases enhances antitumor effects in prostate cancer by decreasing activated survival pathways. PLoS One 7(12), e51189 (2012).

    5. Huang, F., Chang, H., Greer, A., et al. IRS2 copy number gain, KRAS and BRAF mutation status as predictive biomarkers for response to the IGF-1R/IR inhibitor BMS-754807 in colorectal cancer cell lines. Mol. Cancer Ther. 14(2), 620-630 (2014).