G007-LK

G007-LK 구조식 이미지
카스 번호:
1380672-07-0
상품명:
G007-LK
동의어(영문):
G007-LK;CS-1659;G007 LK;G007LK;G007-LK;G007 LK;G007LK;Tankyrase 1/2 Inhibitor VI, G007-LK - Calbiochem;G007LK,Inhibitor,poly ADP ribose polymerase,G-007-LK,G007 LK,PARP,inhibit,G007-LK;(E)-4-(5-(2-(4-(2-chlorophenyl)-5-(5-(methylsulfonyl)pyridin-2-yl)-4H-1,2,4-triazol-3-yl)vinyl)-1,3,4-oxadiazol-2-yl)benzonitrile;4-[5-[(1E)-2-[4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]benzonitrile;Benzonitrile, 4-[5-[(1E)-2-[4-(2-chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl]ethenyl]-1,3,4-oxadiazol-2-yl]-
CBNumber:
CB32707548
분자식:
C25H16ClN7O3S
포뮬러 무게:
529.96
MOL 파일:
1380672-07-0.mol

G007-LK 속성

끓는 점
817.3±75.0 °C(Predicted)
밀도
1.47±0.1 g/cm3(Predicted)
저장 조건
+2C to +8C
용해도
≥26.5 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
물리적 상태
백색분말
산도 계수 (pKa)
-1.68±0.10(Predicted)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
그림문자(GHS): GHS hazard pictograms
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H301 삼키면 유독함 급성 독성 물질 - 경구 구분 3 위험 GHS hazard pictograms P264, P270, P301+P310, P321, P330,P405, P501
예방조치문구:
P301+P310 삼켰다면 즉시 의료기관(의사)의 진찰을 받으시오.

G007-LK C화학적 특성, 용도, 생산

일반 설명

A cell-permeable, triazolyl-vinyl-oxadiazole compound that targets adenosine site of the NAD+ pocket in the TNKS PARP domain and acts as a potent and highly selective tankyrase inhibitor (IC50 = 33 and 26 nM, respectively, against TNKS1/PARP5a/ARTD5 and TNKS2/PARP5b/ARTD6 in auto-PARsylation assays), effectively inhibiting murine Wnt3a-induced reporter activity in human HEK293 and murine 10T1/2 cultures (ICmax ~300 and 600 nM, respectively). Shown to display little or no inhibitory potency (IC50 >10 μM) toward 7 other PARP enzymes (PARP1, 2, 3, 6, 7,10,11), 90 kinases, 16 phosphatases, and 75 GPCRs (IC50 >10 μM). Shown to inhibit two CRC lines, COLO-320DM & SW403, colony formation in vitro (200 nM) and tumor expansion in mice in vivo (20 mg/kg via daily i.p.), although G007-LK toxicity is observed at higher dosages (≥30 mg/kg/12 h or 60 mg/kg/d via i.p.).

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Biochem/physiol Actions

Cell permeable: yes

G007-LK 준비 용품 및 원자재

원자재

준비 용품


G007-LK 공급 업체

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Aladdin Scientific
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