카르필조밉

한글명:카르필조밉

카스 번호868540-17-4

상품명:Carfilzomib

CBNumberCB12520831

분자식C40H57N5O7

포뮬러 무게719.92

MOL 파일868540-17-4.mol

동의어(한글)

카르필조밉

화학적 성질

녹는점	204 - 208°C
끓는 점	975.6±65.0 °C(Predicted)
밀도	1.161
인화점	543.8℃
저장 조건	-20°
용해도	DMSO(최대 80mg/ml) 또는 에탄올(최대 25mg/ml)에 용해됩니다.
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	13.17±0.46(Predicted)
색상	하얀색
안정성	제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO 또는 에탄올 용액은 -20°에서 최대 1주일 동안 보관할 수 있습니다.
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 데이터베이스	868540-17-4

위험 및 안전 성명

HS 번호

29337900

그림문자(GHS)

카르필조밉 화학적 특성, 용도, 생산

개요
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.
화학적 성질
White Solid
용도
Carfilzomib is a second-generation proteasome inhibitor that is used as a treatment in relapsed and refractory multiple myeloma.
정의
ChEBI: Carfilzomib is a synthetic tetrapeptide consisting of morpholin-4-acetyl, L-2-amino-4-phenylbutanoyl, L-leucyl and L-phenylalanyl residues joined in sequence with the C-terminus connected to the amino group of (2<element S)-2-amino-4-methyl-1-[(2R)-2-methyloxiran-2-yl]-1-oxopentan-1-one via an amide linkage. Used for the treatment of patients with multiple myeloma.
Clinical Use
Carfilzomib is an irreversible inhibitor of the chymotrypsin-like protease in the proteasome and was approved in the U.S. for the treatment of multiple myeloma. Carfilzomib was discovered by Proteolix which was later acquired by Onyx Therapeutics who completed the development of this drug. Carfilzomib is also undergoing clinical evaluation for additional oncology indications such as relapsed solid tumors, lymphoma, prolymphocytic leukemia, acute myeloid leukemia and acute lymphocytic leukemia.

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