An inhibitor of HER2
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Tucatinib

Item No. 31411

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N6-(4,5-dihydro-4,4-dimethyl-2-oxazolyl)-N4-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-4,6-quinazolinediamine
CAS Number
937263-43-9
Synonyms
  • ARRY-380
  • ONT-380
Molecular Formula
C26H24N8O2
Formula Weight
480.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml
λmax
214, 244 nm
SMILES
CC1=CC(NC2=C3C=C(NC4=NC(C)(C)CO4)C=CC3=NC=N2)=CC=C1OC5=CC6=NC=NN6C=C5
InChi Code
InChI=1S/C26H24N8O2/c1-16-10-17(5-7-22(16)36-19-8-9-34-23(12-19)28-15-30-34)31-24-20-11-18(4-6-21(20)27-14-29-24)32-25-33-26(2,3)13-35-25/h4-12,14-15H,13H2,1-3H3,(H,32,33)(H,27,29,31)
InChi Key
SDEAXTCZPQIFQM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

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    Product Description

    Tucatinib is an inhibitor of HER2 (IC50 = 14 nM).1 It inhibits the phosphorylation of HER2 in BT474 breast carcinoma cells (IC50 = 21 nM). Tucatinib inhibits phosphorylation of AKT and induces apoptosis in BT474 cells. In vivo, tucatinib (25-100 mg/kg) inhibits tumor growth in NCI N87 gastric carcinoma and SKOV3 ovarian adenocarcinoma mouse xenograft models. Tucatinib also reduces intratumor phosphorylation of AKT and ERK and inhibits tumor growth in a BT474 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pheneger, T., Bouhana, K., Anderson, D., et al. Abstract #1795: In vitro and in vivo activity of ARRY-380: A potent, small molecule inhibitor of ErbB2. AACR Cancer Res. 69(9), 1795 (2009).