Tucatinib (Irbinitinib, ONT-380) - Moligand™, 10mM in DMSO , Receptor protein-tyrosine kinase erbB-2 inhibitor, CAS No.937263-43-9, Receptor protein-tyrosine kinase erbB-2 inhibitor

CAS: 937263-43-9 Cat. No.: T408502 Molecular Weight: 480.52 EC Number: 876-089-2 PubChem CID: 51039094

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

ARRY-380 | 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]​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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 ~5
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

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).
Cell Data

cell lines：Human vascular endothelial cells (HUVECs)

Concentrations：

Incubation Time：

Powder Purity:≥97%

Specifications

Synonyms

ARRY-380 | 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]​-

Specifications & Purity

Moligand™, 10mM in DMSO

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

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Receptor protein-tyrosine kinase erbB-2 inhibitor

Product Properties

• ALogP: 4.744
• HBD Count: 2
• Rotatable Bond: 6

Names and Identifiers

• 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

Associated Targets(Human)

MYH14 Tchem Myosin-14 (1 Activities)

Discover Target: MYH14

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 51 mg/mL (200.65 mM); Ethanol: 51 mg/mL (200.65 mM); Water: Insoluble
• DMSO(mg / mL) Max Solubility: 96
• DMSO(mM) Max Solubility: 199.7835678
• Water(mg / mL) Max Solubility: ＜1