Carfilzomib (PR-171)

产品编号: DC1002 Featured
Carfilzomib (PR-171)
结构式
868540-17-4
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应用领域
Carfilzomib是不可逆的蛋白酶体 (proteasome) 抑制剂,其在ANBL-6和RPMI 8226细胞中的 IC50 为5 nM。
Cas No.: 868540-17-4
名称: L-Phenylalaninamide, (αS)-α-[[2-(4-morpholinyl)acetyl]amino]benzenebutanoyl-L-leucyl-N-[(1S)-3-methyl-1-[[(2R)-2-methyl-2-oxiranyl]carbonyl]butyl]-
别名: PR171,PR 171
SMILES: CC(C)C[C@@H](C(=O)[C@]1(CO1)C)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC3=CC=CC=C3)NC(=O)CN4CCOCC4
分子式: C40H57N5O7
分子量: 719.91
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: In votro:Carfilzomib inhibits proliferation in a variety of cell lines and patient-derived neoplastic cells, including multiple myeloma, and induced intrinsic and extrinsic apoptotic signaling pathways and activation of c-Jun-N-terminal kinase (JNK). Carfilzomib reveals enhanced anti-MM activity compared with bortezomib, overcome resistance to bortezomib and other agents, and acts synergistically with dexamethasone (Dex). Carfilzomib shoes preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, with over 80% inhibition at doses of 10 nM. Short exposure to low-dose Carfilzomib leads to preferential binding specificity for the β5 constitutive 20S proteasome and the β5i immunoproteasome subunits. Measurement of caspase activity in ANBL-6 cells pulsed with Carfilzomib reveals substantial increases in caspase-8, caspase-9, and caspase-3 activity after 8 hours, giving a 3.2-, 3.9- and 6.9-fold increase, respectively, over control cells after 8 hours. In carfilzomib pulse-treated cells, the mitochondrial membrane integrity is decreased to 41% (Q1 + Q2), compared with 75% in vehicle-treated control cells.In another study, Carfilzomib has also shown preclinical effectiveness against hematological and solid malignancies.Carfilzomib directly inhibits osteoclasts formation and bone resorption. In vivo :Carfilzomib moderately reduces tumor growth in an in vivo xenograft model. Carfilzomib effectively decreases multiple myeloma cell viability following continual or transient treatment mimicking. Carfilzomib increases trabecular bone volume, decreases bone resorption and enhances bone formation in non-tumor bearing mice. For the detailed information about the solubility of Carfilzomib (PR-171) in water, the solubility of Carfilzomib (PR-171) in DMSO, the solubility of Carfilzomib (PR-171) in PBS buffer, the animal experiment(test) of Carfilzomib (PR-171),the in vivo,in vitro and clinical trial test of Carfilzomib (PR-171),the cell experiment(test) of Carfilzomib (PR-171),the IC50, EC50 and Affinity of Carfilzomib (PR-171), please contact DC Chemicals.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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DC2010 Oprozomib (ONX-0912) Oprozomib (ONX 0912; PR047)是口服生物相容性的抑制剂,能抑制20S proteasome(20S蛋白酶体)β5/LMP7的CT-L活性,IC50为36 nM/82 nM。
DC1027 Bortezomib (Velcade,MG-341,PS-341) Bortezomib (PS-341) 是一种可逆性和选择性的蛋白酶体抑制剂,通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki=0.6 nM)。Bortezomib 破坏细胞周期、诱导细胞凋亡以及抑制核因子 NF-κB。Bortezomib 具有抗肿瘤活性。
DC1002 Carfilzomib (PR-171) Carfilzomib是不可逆的蛋白酶体 (proteasome) 抑制剂,其在ANBL-6和RPMI 8226细胞中的 IC50 为5 nM。