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DS-1205b free base - 10mM in DMSO , CAS No.1855860-24-0
주문 가능
등급 & 순도 10mM in DMSO
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
이 등급을 선택하는 이유
10mM in DMSO 최소한의 기준선 간섭이 필요한 민감한 크로마토그래피 및 분석 워크플로우용.
보관 및 배송
Store at -80°C Dry ice packs + Cold packs 출고. 정확한 사양은 로트별 COA를 확인하세요.
품질 문서
SDS, COA, 데이터시트, 사양서를 다운로드할 수 있습니다. 로트별 COA는 로트 번호 조회를 통해 확인할 수 있습니다.
문헌적 근거
크로마토그래피, 유기 합성 및 교차 커플링 반응 분야의 동료 심사 논문 0편에서 인용되었습니다.
개요
DS-1205b free base is a potent and selective inhibitor of AXL kinase , with an IC 50 of 1.3 nM. DS-1205b free base also inhibits MER , MET , and TRKA , with IC 50 s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo
In Vitro
DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC 50 =2.7 nM). DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI 50 >10,000 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: NIH3T3-AXL cells Concentration: 1, 10, 100, 1000, 10000 μM Incubation Time: 2, 24 hours Result: Completely inhibited the phosphorylation of AXL at concentrations above 10 nM. Slightly inhibited the phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.
In Vivo
DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks Dosage: 3.1, 6.3, 13, 25, 50 mg/kg Administration: P.o. twice daily for 5 days Result: Inhibited tumor growth by 39-94%. Reduced the phosphorylation of both AXL and AKT in tumors.
IC50& Target:AXL 1.3 nM (IC 50 ) MER 63 nM (IC 50 ) TrkA 407 nM (IC 50 ) Met 104 nM (IC 50 )
사양
사양 및 순도
10mM in DMSO
생화학 및 생리적 메커니즘
DS-1205b free base is a potent and selective inhibitor of AXL kinase , with an IC 50 of 1.3 nM. DS-1205b free base also inhibits MER , MET , and TRKA , with IC 50 s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vit
보관 조건
Store at -80°C
배송
Dry ice packs + Cold packs
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작업 유형
INHIBITOR
이름과 식별자
PubChem CID
129110632
분자량
735.80
문서
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