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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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T413986-5mg | 5mg | In stock | $35.90 | |
T413986-25mg | 25mg | In stock | $148.90 | |
T413986-50mg | 50mg | In stock | $246.90 | |
T413986-100mg | 100mg | In stock | $444.90 |
HER2/ErbB2 Selective Inhibitors
Synonyms | Tucatinib|Irbinitinib|937263-43-9|Tukysa|ONT-380|6-DIAMINE|Arry 380|N6-(4,4-Dimethyl-4,5-dihydrooxazol-2-yl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)quinazoline-4,6-diamine|UNII-234248D0HH|ONT 380|Irbinitinib(ARRY-380)|234248D0HH|Irbi |
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Specifications & Purity | Moligand™, ≥96% |
Biochemical and Physiological Mechanisms | Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor of ErbB-2 (also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Receptor protein-tyrosine kinase erbB-2 inhibitor |
Product Description | Information Tucatinib (Irbinitinib, ONT-380, ARRY-380) is an oral, potent, selective, reversible and ATP-competitive small-molecule inhibitor ofErbB-2(also called HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively in cell-based assays, showing ~500-fold selective for HER2 vs EGFR. It has potential antineoplastic activity. Targets p95 HER2 (Cell-based assay); ErbB2 (Cell-based assay) 7 nM; 8 nM In vitro The compound is a reversible, ATP-competitive inhibitor with nanomolar potency against ErbB2 in both in vitro and in cell-based assays. Incell-based assays, ARRY-380 is ~500-fold selective for HER2 vs. EGFR and is equipotent against truncated p95-HER2. In vivo ARRY-380 significantly inhibits tumor growth in multiple HER2-dependent tumor xenograft models. It shows excellent 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, ARRY-380 demonstrated significant dose-related tumor growth inhibition (TGI; 50% at 50 mg/kg/d and 96% at 100 mg/kg/d) with numerous partial regressions (>50% reduction from baseline size). |
ALogP | 4.744 |
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HBD Count | 2 |
Rotatable Bond | 6 |
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IUPAC Name | 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 |
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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) |
InChi Key | SDEAXTCZPQIFQM-UHFFFAOYSA-N |
Canonical SMILES | CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5 |
Isomeric SMILES | CC1=C(C=CC(=C1)NC2=NC=NC3=C2C=C(C=C3)NC4=NC(CO4)(C)C)OC5=CC6=NC=NN6C=C5 |
PubChem CID | 51039094 |
Molecular Weight | 480.52 |
CAS Registry No. | 937263-43-9 |
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PubChem CID | 51039094 |
DrugCentral Ligand | 5389 |
Enter Lot Number to search for COA:
To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section
Lot Number | Certificate Type | Date | Item |
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K2218811 | Certificate of Analysis | Jul 21, 2022 | T413986 |
K2218898 | Certificate of Analysis | Jul 21, 2022 | T413986 |
K2218976 | Certificate of Analysis | Jul 21, 2022 | T413986 |
K2218987 | Certificate of Analysis | Jul 21, 2022 | T413986 |
Solubility | Solubility (25°C) In vitro DMSO: 96 mg/mL (199.78 mM); Water: Insoluble; Ethanol: Insoluble; |
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DMSO(mg / mL) Max Solubility | 96 |
DMSO(mM) Max Solubility | 199.7835678 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
1. Moulder SL, Borges VF, Baetz T, Mcspadden T, Fernetich G, Murthy RK, Chavira R, Guthrie K, Barrett E, Chia SK. (2017) Phase I Study of ONT-380, a HER2 Inhibitor, in Patients with HER2+-Advanced Solid Tumors, with an Expansion Cohort in HER2+ Metastatic Breast Cancer (MBC).. Clin Cancer Res, 23 (14): (3529-3536). [PMID:28053022] |
2. Kulukian A, Lee P, Taylor J, Rosler R, de Vries P, Watson D, Forero-Torres A, Peterson S. (2020) Preclinical Activity of HER2-Selective Tyrosine Kinase Inhibitor Tucatinib as a Single Agent or in Combination with Trastuzumab or Docetaxel in Solid Tumor Models.. Mol Cancer Ther, 19 (4): (976-987). [PMID:32241871] |