insoluble in H2O; ≥51.5 mg/mL in DMSO; ≥51.6 mg/mL in EtOH
물리적 상태
결정성 고체
산도 계수 (pKa)
10.92±0.50(Predicted)
안전
위험 및 안전 성명
위험 및 사전주의 사항 (GHS)
그림문자(GHS):
신호 어:
Warning
유해·위험 문구:
암호
유해·위험 문구
위험 등급
범주
신호 어
그림 문자
P- 코드
H320
눈에 자극을 일으킴
심한 눈 손상 또는 자극성 물질
구분 2B
경고
P264, P305+P351+P338,P337+P313
예방조치문구:
P264
취급 후에는 손을 철저히 씻으시오.
P264
취급 후에는 손을 철저히 씻으시오.
P305+P351+P338
눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
P337+P313
눈에 대한 자극이 지속되면 의학적인 조치· 조언를 구하시오.
NFPA 704
0
1
0
AZD3965 C화학적 특성, 용도, 생산
개요
AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1; Ki = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport. It displays six-fold selectivity for MCT1 over MCT2 and is without effect against MCT4 at 10 μM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts. AZD 3965 also enhances radiosensitivity in mice with SCLC xenografts.
효소 저해제
This orally bioavailable MCT1 inhibitor (FW = 515.51 g/mol; CASs =
733809-45-5 and 1448671-31-5), also named (S) -5- (4-hydroxy-4-
methylisoxazolidine-2-carbonyl) -1-isopropyl-3-methyl-6- ( (3-methyl-5- (tri-
fluoromethyl) -1H-pyrazol-4-yl) methyl) -thieno[2,3-d]pyrimidine-2,4 (1H,
3H) -dione, selectively targets the Monocarboxylate Transporter-1 (IC50 =
1.6 nM) and is ~6x less active toward MCT2. AZD3965 does not inhibit
MCT4, even at 10 μM. MCT1 and MCT4 are primarily involved in lactate
transport, targeting highly glycolytic cancer cells, especially those that are
hypoxic. The latter property suggests that the combined use with a
vascular-disrupting anticancer agent (such as combrestatin) may improve
the inhibitory action of AZD-3965 against cancer cells.
