Home Categories Biochemical Engineering Carfilzomib
A2463112

Carfilzomib , ≥99% , 868540-17-4

CAS NO.:868540-17-4

Empirical Formula: C40H57N5O7

Molecular Weight: 719.92

MDL number: MFCD11040997

EINECS: 692-054-2

Pack Size Price Stock Quantity
5MG RMB111.20 In Stock
10MG RMB175.20 In Stock
25MG RMB302.40 In Stock
50MG RMB599.20 In Stock
100MG RMB903.20 In Stock
500mg RMB2799.20 In Stock
others     Enquire
Update time: 2022-07-08

PRODUCT Properties

Melting point: 204 - 208°C
Boiling point: 975.6±65.0 °C(Predicted)
Density  1.161
Flash point: 543.8℃
storage temp.  -20°
solubility  Soluble in DMSO (up to 80 mg/ml) or in Ethanol (up to 25 mg/ml).
form  solid
pka 13.17±0.46(Predicted)
color  White
Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 1 week.
InChIKey BLMPQMFVWMYDKT-KWQOZBPPNA-N
SMILES C([C@@]1(OC1)C)(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)CN1CCOCC1)CCC1C=CC=CC=1)CC1C=CC=CC=1 |&1:1,6,14,18,26,r|
CAS DataBase Reference 868540-17-4

Description and Uses

In July 2012, the US FDA approved carfilzomib (also referred to as PR-171) for the treatment of patients with multiple myeloma (MM) who have received at least two prior therapies including bortezomib and an immunomodulatory agent and have demonstrated disease progression within 60 days of completion of the last therapy. Carfilzomib binds to and irreversibly inhibits the chymotrypsin-like protease activity of the constitutive proteosome (β5) and immunoproteosome (β5i) via its epoxyketone pharmacophore. Proteosome inhibition results in the accumulation of polyubiquitinated proteins and induction of apoptosis through activation of both the intrinsic and extrinsic caspase pathways. Carfilzomib inhibits chymotrypsin activity with an IC50 of 6 nM and is less potent an inhibitor of trypsin and caspase (IC50s of 3600 and 2400 nM, respectively). Cell cycle arrest and apoptosis are seen in a variety of hematologic and solid tumor cell lines (e.g.,MM, acutemyeloid leukemia (AML), pancreatic cancer, lung cancer) treated with carfilzomib.

Carfilzomib is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma.

Safety

Symbol(GHS) 
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P305+P351+P338
HS Code  29337900

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