Carfilzomib , ≥99% , 868540-17-4

CAS NO.：868540-17-4

Empirical Formula: C40H57N5O7

Molecular Weight: 719.92

MDL number: MFCD11040997

EINECS: 692-054-2

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.

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 (IC_50s 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