Tucatinib | B3025

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.

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.

B3025 | Tucatinib DataSheet

Alternate Name/Synonyms: 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

Appearance: White to off-white solid powder

Formulation:

CAS Number: 937263-43-9

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₂₆H₂₄N₈O₂

Molecular Weight: 480.52

Cell-Permeable?: TRUE

Purity: ≥97%

Solubilities: ~50 mg/ml in DMSO (may need ultrasonication)

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: An inhibitor of ErbB2 (HER2)

MDL Number: MFCD22380467

PubChem CID: 51039094

SMILES: CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5

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)

InChi Key: SDEAXTCZPQIFQM-UHFFFAOYSA-N