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Carfilzomib, Proteasome Inhibitor

Carfilzomib, Proteasome Inhibitor

$109.00
A selective, irreversible proteasome inhibitor.
Catalog No. Unit Price Qty
M60109-2s 2 mg solid $109.00
M60109-2 2 mg solid $109.00

Details

Product Information
Chemical Name: (S)-4-methyl-N-((S)-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide
Molecular Weight: 719.91
Formula: C40H57N5O7
Purity: ≥ 98%
CAS#: 868540-17-4
Solubility: DMSO up to 100 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year

Biological Activity:

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.


How to Use:

  • In vitro: Carfilzomib was used at 0.1 µM in vitro and in cellular assays.
  • In vivo: Carfilzomib was dosed to mice/rats by intravenous administration at 0.5-4 mg/kg once per day.


Reference:

  1. 1. Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. (2007) Blood. 110(9):3281-90.
  2. 2. Parlati F,et al. Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome. (2009) Blood.114(16):3439-47.
  3. 3. Dasmahapatra G, et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo. (2011) Mol Cancer Ther. 10(9):1686-97.
  4. 4. Sacco A, et al. Carfilzomib-dependent selective inhibition of the chymotrypsin-like activity of the proteasome leads to antitumor activity in Waldenstrom's Macroglobulinemia. (2011) Clin Cancer Res. 17(7):1753-64.



Products are for research use only. Not for human use.

Description

Details

Product Information
Chemical Name: (S)-4-methyl-N-((S)-1-(((S)-4-methyl-1-((R)-2-methyloxiran-2-yl)-1-oxopentan-2-yl)amino)-1-oxo-3-phenylpropan-2-yl)-2-((S)-2-(2-morpholinoacetamido)-4-phenylbutanamido)pentanamide
Molecular Weight: 719.91
Formula: C40H57N5O7
Purity: ≥ 98%
CAS#: 868540-17-4
Solubility: DMSO up to 100 mM
Storage: Powder: 4oC 1 year DMSO: 4oC 3 month -20oC 1 year

Biological Activity:

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.


How to Use:

  • In vitro: Carfilzomib was used at 0.1 µM in vitro and in cellular assays.
  • In vivo: Carfilzomib was dosed to mice/rats by intravenous administration at 0.5-4 mg/kg once per day.


Reference:

  1. 1. Kuhn DJ, et al. Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. (2007) Blood. 110(9):3281-90.
  2. 2. Parlati F,et al. Carfilzomib can induce tumor cell death through selective inhibition of the chymotrypsin-like activity of the proteasome. (2009) Blood.114(16):3439-47.
  3. 3. Dasmahapatra G, et al. Carfilzomib interacts synergistically with histone deacetylase inhibitors in mantle cell lymphoma cells in vitro and in vivo. (2011) Mol Cancer Ther. 10(9):1686-97.
  4. 4. Sacco A, et al. Carfilzomib-dependent selective inhibition of the chymotrypsin-like activity of the proteasome leads to antitumor activity in Waldenstrom's Macroglobulinemia. (2011) Clin Cancer Res. 17(7):1753-64.



Products are for research use only. Not for human use.

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