Carfilzomib --- Proteasome Inhibitor
| Overview | |
| Catalog # | bs-60109c-2-mg-solid |
| Product Name | Carfilzomib --- Proteasome Inhibitor |
| Specifications | |
| Storage Buffer | Powder |
| Storage Condition | Store in dry, dark place at -20C for 1 year. |
| Target | |
| Product Information | Molecular Weight: 719.91 Formula: C40 H57 N5 O7 CAS Number: 868540-17-4 InChi Key: BLMPQMFVWMYDKT-NZTKNTHTSA-N InChi: InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1 Smiles: C[C@@]1(CO1)C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1C=CC=CC=1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC1C=CC=CC=1)NC(=O)CN1CCOCC1 Purity: 98.0 Solubility: DMSO up to 100 mM Appearance: Solid Power. Shelf Life: 1.0 years |
| Description | Carfilzomib is a selective, irreversible proteasome inhibitor (over 80% inhibition at doses of 10 nM and above). In models of multiple myeloma, Carfilzomib potently bound and specifically inhibited the chymotrypsin-like proteasome and immunoproteasome activities, resulting in accumulation of ubiquitinated substrates. It induced a dose- and time-dependent inhibition of proliferation, ultimately leading to apoptosis. It also inhibited proliferation and activated apoptosis in patient-derived MM cells and neoplastic cells from patients with other hematologic malignancies. Carfilzomib showed increased efficacy compared with bortezomib and was active against bortezomib-resistant MM cell lines and samples from patients with clinical bortezomib resistance. Currently it is approved by US FDA for relapsed and refractory multiple myeloma in 2012. |
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