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抑制剂/激活剂

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凋亡与自噬

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Carfilzomib (PR-171)

Carfilzomib (PR-171) 卡非佐米

Carfilzomib (PR-171) 是一种不可逆proteasome抑制剂，在ANBL-6细胞中IC50为<5 nM，在体外优先抑制β5亚基的ChT-L活性，对PGPH和T-L活性很弱或没有作用。Carfilzomib 可激活自噬并诱导细胞凋亡。

货号：
TK0332
规格：

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	868540-17-4
生物活性	Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
分子式	C40H57N5O7
分子量	719.91
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder, -20°C ,3 years
溶解性数据	DMF : ≥ 100 mg/mL (138.91 mM)，DMSO : 50 mg/mL (69.45 mM; Need ultrasonic)
体内研究	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.
体外研究	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 IC50 of 15.2 nM, less than the value of 29.3 nM for parental MM1.S cells. 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.
纯度及产品资料	98%

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