Carfilzomib;PR171 868540-17-4
| 1.Inquiries will be replied within 24 hours |
| 2.We could supply various packages as you required |
| 3.To protect the profit of our agents, price will not show on website, please send inquiries to get the price. |
| 4.Fast delivery, goods arrive your office within 3 to 5 days |
| 5.Please click "Inquiry" or "Email" below to get the price |
|
|
|
|
white powder |
|
|
C40H57N5O7 |
|
|
|
|
719.91 |
|
in stock |
|
|
868540-17-4 |
|
99.5% |
Introduction
Carfilzomib is an irreversible proteasome inhibitor with IC50 of < 5 nM in ANBL-6 and RPMI 8226 cells. IC50 & Target: IC50: 5 nM (Proteasome) In Vitro: Carfilzomib displays preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM and above and little or no effect on the PGPH and T-L activities at doses up to 100 nM. Carfilzomib decreases the viability of ANBL-6, RPMI 8226 cells, U266 and KAS-6/1 cells with an IC50 less than 5 nM. Carfilzomib overcome Dex resistance, in that MM1.R cells reveals an IC50of 15.2 nM, less than the value of 29.3 nM for parental MM1.S cells[1]. Co-treatment with carfilzomib and HDACIs leads to synergistic induction of cell death in various mantle cell lymphoma lines and primary mantle cell lymphoma cells. Combined treatment with carfilzomib or ONX0912 with vorinostat in HF-4B and Granta cells sharply increases caspase activation, PARP cleavage, JNK activation, MnSOD2 induction, and DNA damage[2]. In Vivo: Carfilzomib (2.0 mg/kg, i.v.) in conbination with 70 mg/kg vorinostat virtually abrogates tumor growth in Granta-luciferace cell xenograft flank model. Combined treatment results in a pronounced reduction in bioluminescence compared to animals treated with single agents or controls with minimal toxicity[2].
