| CAS NO: | 148741-30-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 10mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
| 250mg | 询价 |
| 500mg | 询价 |
| 1g | 询价 |
| Molecular Weight (MW) | 316.46 |
|---|---|
| Formula | C18H24N2OS |
| CAS No. | 148741-30-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 36 mg/mL (113.7 mM) |
| Water: <1 mg/mL | |
| Ethanol: 3 mg/mL (9.5 mM) | |
| Solubility (In vivo) | 1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL |
| Synonyms | AG 879; Tyrphostin AG 879; Tyrphostin AG879; Tyrphostin AG-879; AG879; AG-879; Chemical Name: 2-Propenethioamide, 3-(3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl)-2-cyano-, (E)- InChi Key: XRZYELWZLNAXGE-KPKJPENVSA-N InChi Code: InChI=1S/C18H24N2OS/c1-17(2,3)13-8-11(7-12(10-19)16(20)22)9-14(15(13)21)18(4,5)6/h7-9,21H,1-6H3,(H2,20,22)/b12-7+ SMILES Code: S=C(N)/C(C#N)=C/C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 |
| In Vitro | In vitro activity: 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). Kinase Assay: TyrphostinAG879 is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation, but not TrKB and TrKC. It is also a ErbB2 kinase inhibitor, has at least 500-fold higher selectivity to ErbB2 (IC50 = 1 μmol/L) than EGFR (IC50>500 μmol/L). Cell Assay: MCF-7 cells are grown in 96-well plates containing 100 μL 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 μL 10% SDS in 0.01 M HCl is added. After incubation at 37°C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm. |
|---|---|
| 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. |
| Animal model | Nude mice bearing v-Ha-RAS transformed NIH 3T3 cells |
| Formulation & Dosage | Dissolved in 30% DMSO with PBS; 20 mg/kg; i.p. injection |
| References | Cancer Res. 2005 Jul 1;65(13):5848-56; Anticancer Drugs. 2006 Sep;17(8):929-41. |
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