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Cat No.: 1092578-46-5
Biological Description:Tofacitinib(CP-690550) is a novel inhibitor of JAK3 with IC50 of 1 nM, 20- to 100-fold less potent against JAK2 and JAK1.IC50 value: 1 nM [1]Target: JAK3in vitro: CP-690550 is a specific, orally inhibitor of JAK3, it is 20- to 100-fold less potent for JAK2 and JAK1 with IC50 of 20 nM and 112 nM, respectively. CP-690550 doesn"t have potent activity against 30 other kinases (all median IC50 > 3000 nM). CP-690,550 inhibits IL-2–induced proliferation with 30-fold greater potency than its effects on GM-CSF–induced proliferation [1]. CP-690550 effectively inhibits a murine mixed lymphocyte reaction (MLR) (IC50 = 91 nM) [2]. CP-690550 potently inhibits IL-4 induced upregulation of CD23 (IC50=57 nM) and class II major histocompatibility complex (MHCII) expression (IC50=71 nM) on murine B cells [3]. in vivo: In a murine model of heterotopic heart transplantation (DBA2 donor heart into C57/BL6 host), CP-690550 results in a dose-dependent increase in survival of transplanted hearts.The EC50 (drug concentrati...Purity: >98%Molecular formula: C16H20N6OMolecular Weight: 312.37Storage Instructions: Two years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSOReferences: for more information, please visit images/AffixScientific/ Affix Scientific的KRN633是一种有效的选择性VEGFR抑制剂。抑制人脐静脉内皮细胞中VEGFR-2的酪氨酸磷酸化(IC50 = 1.16 nmol / L)。用重组酪氨酸激酶进行的选择性分析表明,KRN633对VEGFR-1,-2和-3具有高度选择性。在无胸腺小鼠和大鼠中,KRN633在几种具有不同组织起源的体内肿瘤异种移植模型(包括肺,结肠和前列腺)中抑制肿瘤生长。KRN633还可以使一些公认的肿瘤以及那些在停止治疗后已长出的肿瘤消退。KRN633具有良好的耐受性,对动物的体重或总体健康没有明显影响。KRN633可用于治疗实体瘤和其他依赖病理性血管生成的疾病。