A pan-inhibitor of HER and VEGFR family kinases
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BMS 690514

Item No. 44552

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]-3-piperidinol
CAS Number
859853-30-8
Molecular Formula
C19H24N6O2
Formula Weight
368.4
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Water (1:1): Slightly soluble: 0.1-1 mg/ml
SMILES
COC1=CC=CC(NC2=NC=NN(C=C3)C2=C3CN4CC[C@H]([C@@H](C4)O)N)=C1
InChi Code
InChI=1S/C19H24N6O2/c1-27-15-4-2-3-14(9-15)23-19-18-13(5-8-25(18)22-12-21-19)10-24-7-6-16(20)17(26)11-24/h2-5,8-9,12,16-17,26H,6-7,10-11,20H2,1H3,(H,21,22,23)/t16-,17-/m1/s1
InChi Key
CSGQVNMSRKWUSH-IAGOWNOFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BMS 690514 is a pan-inhibitor of HER and VEGFR family kinases (IC50s = 5, 19, 60, 50, 50, and 25 nM for EGFR, HER2, HER4, VEGFR1, VEGFR2, and VEGFR3, respectively).1 It is selective for these kinases over 11 additional kinases but also inhibits FMS-related tyrosine kinase 3 (FLT3), calcium/calmodulin-dependent protein kinase II (CAMKII), LCK, and PKA (IC50s = 110, 170, 220, and 280 nM, respectively). BMS 690514 selectively inhibits the proliferation of cancer cells containing EGFR gene amplifications or mutations and HER2 gene amplifications over those expressing wild-type EGFR or not expressing EGFR and HER2. It inhibits tumor growth and angiogenesis in an L2987 lung cancer mouse xenograft model when administered at a dose of 90 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wong, T.W., Lee, F.Y., Emanuel, S., et al. Antitumor and antiangiogenic activities of BMS-690514, an inhibitor of human EGF and VEGF receptor kinase families. Clin. Cancer Res. 17(12), 4031-4041 (2011).