Tyrphostin AG 879 - Moligand™, 10mM in DMSO , CAS No.148741-30-4

CAS: 148741-30-4 Cat. No.: T408845 Molecular Weight: 316.46 EC Number: 878-915-7 PubChem CID: 135419190

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

AG 879 | 2-Propenethioamide, 3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-, (2E)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Tyrphostin AG 879 Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
In vitro

AG879 inhibits growth of FET6αS26X cells in a concentration-dependent manner. AG879(10 nM) blocks the activation of PAK1 and suppresses RAS-induced malignant transformation of NIH 3T3 cells. AG879(<1 μM) inhibits the Tyr-phosphorylation of ERK and its association with PAK1 in v-Ha-RAS-transformed NIH 3T3 fibroblasts. AG 879 dose-dependently reduce MCF-7 cell numbers and show already a significant effect at 0.4 mM through inhibiting DNA synthesis and mitotic. AG 879(<20 μM) inhibits activation of ERK-1/2 in MCF-7 cell. AG 879(5 μM) decreases expression of Hsp90 client proteins RAF-1 and HER-2. AG879(20 μM) dramatically decreases proliferation with a variable increase in apoptosis in Cell lines from human leiomyosarcoma (HTB-114, HTB-115, HTB-88), rhabdomyosarcoma (HTB-82, TE-671), prostatic adenocarcinoma (PC-3), acute promyelocytic leukemia (HL-60) and histiocytic lymphoma (U-937).

In vivo

AG879(2 mg) induces a decrease in cancer growth in athymic NOD/SCID mice grafted with HTB-114 or HL-60. AG 879(20 mg/kg) treatment keeps 50% of mice absolutely free of RAS-induced sarcomas, and dramatically reduces the size of the growing sarcomas in the nude mice carrying v-Ha-RAS transformed NIH 3T3 cells.
Cell Data

cell lines：Jurkat, Loucy, KOPTK1 and DND-41 cell lines

Concentrations：20 μM

Incubation Time：46 hours

Powder Purity:≥99%

Specifications

Synonyms

AG 879 | 2-Propenethioamide, 3-[3, 5-bis(1, 1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-, (2E)-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.

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™

Names and Identifiers

• Isomeric SMILES: CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)/C=C(\C#N)/C(=S)N
• WGK Germany: 3
• PubChem CID: 135419190
• Molecular Weight: 316.46

Associated Targets(Human)

CYP2C9 Tchem Cytochrome P450 2C9 (1 Activities)

Discover Target: CYP2C9

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

Chemical and Physical Properties

• Refractive Index: 1.61
• Boil Point(°C): ~443.81° C at 760 mmHg
• Melt Point(°C): 219-220°C