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Alternative_name
Irbinitinib; ONT-380; 6-DIAMINE; ARRY-380; 6-N-(4,4-dimethyl-5H-1,3-oxazol-2-yl)-4-N-[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]quinazoline-4,6-diamine; 4,6-QuinazolinediaMine,N6-(4,5-dihydro-4,4-diMethyl-2-oxazolyl)-N4-[3-Methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-; N6-(4,4-dimethyl-1,3-oxazolidin-2-ylidene)-n4-(3-methyl-4-{[1,2,4]triazolo[1,5-a]pyridin-7-yloxy}phenyl)quinazoline-4,6-diamine
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Description
Tucatinib is an oral, potent, selective and ATP-competitive small-molecule inhibitor of Receptor tyrosine-protein kinase ErbB2 (also called HER2 or human epidermal growth factor receptor 2) with an IC₅₀ of 14 nM against ErbB2 enzyme. It inhibits the phosphorylation of ErbB2 in BT474 cells with an IC₅₀ of 21 nM. It shows excellent anti-tumor activity in numerous mouse tumor models including breast (BT-474, MDA-MB-453), ovarian (SKOV-3) and gastric (N87) carcinoma models. In the BT-474 model, it showed significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d). It is approved to be used in combination chemotherapy for advanced HER2-positive breast cancer.
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CAS Number
937263-43-9
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Structure Available
1
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Molecular Formula
C₂₆H₂₄N₈O₂
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Molecular Weight
480.52
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Cell Permeable
1
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Purity
≥97%
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Solubilities
~50 mg/ml in DMSO (may need ultrasonication)
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Handling
Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
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Tag Line
An inhibitor of ErbB2 (HER2)
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Storage Condition
-20ºC
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Shipping Condition
RT
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Shelf Life
36 months
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MDL Number
MFCD22380467
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PubChem CID
51039094
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SMILES
CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5
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InChi
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)
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InChi Key
SDEAXTCZPQIFQM-UHFFFAOYSA-N
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MSDS Available
1
