10-Propargyl-10-deazaaminopterin

한글명:10-Propargyl-10-deazaaminopterin

카스 번호146464-95-1

상품명:10-Propargyl-10-deazaaminopterin

CBNumberCB31856065

분자식C23H23N7O5

포뮬러 무게477.47

MOL 파일146464-95-1.mol

화학적 성질

녹는점	215 °C(dec.)
밀도	1.471±0.06 g/cm3(Predicted)
저장 조건	2-8°C
수용성	물에 불용성
용해도	≥23.85 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
산도 계수 (pKa)	3.53±0.10(Predicted)
물리적 상태	powder to crystal
색상	흰색에서 밝은 노란색

위험 및 안전 성명

HS 번호

2933.59.5300

유해 물질 데이터

146464-95-1(Hazardous Substances Data)

NFPA 704:

	0
2		0

그림문자(GHS)

10-Propargyl-10-deazaaminopterin 화학적 특성, 용도, 생산

개요
Pralatrexate, an injectable DHFR inhibitor, was launched for the treatment of patients with relapsed or refractory PTCL. PTCL is an aggressive form of non-Hodgkin’s lymphoma (NHL) characterized by the proliferation of abnormal T-lymphocytes that circulate in the peripheral bloodstream. The inhibition of the folate enzymes DHFR and thymidylate synthase is a well-validated method of cancer treatment. In vitro, pralatrexate is slightly less potent than MTX in inhibiting DHFR derived from murine leukemia L1210 cells (K_i = 18.2 pM vs. 5.75 pM) and human leukemia CCRF-CEM cells (K_i = 13.4 pM vs. 5.4 pM). However, it is transported into both types of cells with 10-fold higher efficiency than MTX, thereby providing a more potent inhibition of cell growth as compared with MTX. In vivo, intraperitonally administered pralatrexate at 60 mg/ kg twice weekly for three or four doses caused complete lymphoma regressions in 89, 56, and 30% of HT, RL, and SKI-DLBCL-1 xenografted mice, respectively, whereas a similar dosing of MTX at 40 mg/kg twice weekly did not produce complete regression. The posttreatment tumor diameter was also smaller in pralatrexate-treated animals.
용도
An antifolate with high affinity for the reduced folate carrier-type 1, produces marked complete and durable remissions in a diversity of chemotherapy refractory cases of T-cell lymphoma.
정의
ChEBI: A pteridine that is the N-4-[1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl]benzoyl derivative of L-glutamic acid. Used for treatment of Peripheral T-Cell Lymphoma, an aggressive form of non-Hodgkins lymphoma.
Clinical Use
Pralatrexate, an injectable dihydrofolate reductase (DHFR) inhibitor, has a superior potency and toxicity profile compared to other DHFR inhibitors. In 2009, the compound was launched by Allos and approved in the U.S. for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL) as a single agent. It is the first drug approved for this indication.70 In 2010, orphan drug designation was received in the E.U. for the treatment of cutaneous T-cell lymphoma (CTCL).
부작용
The most common adverse reactions associated with pralatrexate are mucositis, thrombocytopenia, nausea, and fatigue. Folic acid and vitamin B12 supplements are administered as adjunct therapies to potentially reduce pralatrexate-related hematological toxicity and mucositis.

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