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Tyrphostin AG 879

Tyrphostin AG 879

Item no.	S2816-5000
Manufacturer	Selleckchem
CASRN	148741-30-4
Amount	5 g
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 25 mg 5 mg 5 g
Category	Oncology Neuroscience Targets for Rodent Neurosciences Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Skin Cancer Breast Cancer Heart & Blood Cancer Lymphatic System Cancer
Type	Inhibitors
Specific against	other
Smiles	CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)C=C(C#N)C(=S)N
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	AG 879
Similar products	Tyrphostin
Available
Manufacturer - Targets	ERBB2
Storage Conditions	2 years -80 in solvent
Molecular Weight	316, 46
Administration	Intraperitoneally administrated on days 3, 5, 7, 10, 12, 14, and 17.
Animal Models	nude mice carrying v-Ha-RAS transformed NIH 3T3 cells
Cell lines	MCF-7 cells
Concentrations	20 uM
Dosages	20 mg/kg
Formulation	30% dimethyl sulfoxide with PBS
IC50	1 M, 1 M, 1 M, 1 M, 1 M, 1 M
In vitro	AG879 inhibits growth of FET6alphaS26X cells in a concentration-dependent manner. [1] AG879(10 nM) blocks the activation of PAK1 and suppresses RAS-induced malignant transformation of NIH 3T3 cells. AG879(<1 uM) inhibits the Tyr-phosphorylation of ERK and its association with PAK1 in v-Ha-RAS-transformed NIH 3T3 fibroblasts. [2] 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 uM) inhibits activation of ERK-1/2 in MCF-7 cell. AG 879(5 uM) decreases expression of Hsp90 client proteins RAF-1 and HER-2. [3] AG879(20 uM) 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). [4]
In vivo	AG879(2 mg) induces a decrease in cancer growth in athymic NOD/SCID mice grafted with HTB-114 or HL-60. [4] 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. [5]
Incubation Time	46 hours
Method	Cells are grown in 96-well plates containing 100 L medium per well. Ten microliters of MTT solution (5 mg/ml in PBS) is added to each well and incubation continued for 4 h at 37 C. Subsequently, 100 L 10% SDS in 0.01 M HCl is added. After incubation at 37C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm.
Solubility (25C)	DMSO 36 mg/mL, Water <1 mg/mL, Ethanol 3 mg/mL
Information	Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
Chemical Name	2-Propenethioamide, 3-[3, 5-bis(1, 1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-, (2E)-

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S2816-5000-datasheet.pdf

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