| 中文名称: | 赛度替尼 | ||||
|---|---|---|---|---|---|
| 英文名称: | Cerdulatinib | ||||
| 别名: | 赛度替尼;塞度替尼;SYK和JAK酶抑制剂(CERDULATINIB);赛度替尼杂质;4-(环丙基氨基)-2-((4-(4-(乙基磺酰基)哌嗪-1-基)苯基)氨基)嘧啶-5-甲酰胺 PRT062070;PRT2070;PRT-062070;PRT-2070;PRT062070;PRT2070;PRT062070(Cerdulatinib);CS-1823;4-(Cyclopropylamino)-2-[[4-[4-(ethylsulfonyl)-1-piperazinyl]phenyl]amino]-5-pyrimidinecarboxamide;Cerdulatinib;PRT-062070;4-(cyclopropylamino)-2-(4-(4-(ethylsulfonyl)piperazin-1-yl)phenylamino)pyrimidine-5-carboxamidePRT062070;Cerdulatinib(PRT-062070 | ||||
| CAS No: | 1198300-79-6 | 分子式: | C20H27N7O3S | 分子量: | 445.54 |
| CAS No: | 1198300-79-6 | ||||
| 分子式: | C20H27N7O3S | ||||
| 分子量: | 445.54 | ||||
熔点：
>211°C (dec.)
沸点：
741.9±70.0 °C(Predicted)
密度：
1.44±0.1 g/cm3(Predicted)
包装规格：
1ml in glass bottle
产品简介：
一种有效和选择性的 Tyk2抑制剂，IC50为0.5 nM。Cerulatinib 也是 JAK 和 SYK 的双重抑制剂，对于 JAK1，JAK2，JAK3和 SYK，IC50分别为12nM，6nM，8nM 和32nM。
溶解性：
DMSO :≥ 30 mg/mL (67.33 mM) "≥" means soluble, but saturation unknown.
储备液保存：
-80°C, 2 years
-20°C, 1 year
体内实验：
1、请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% Saline
Solubility: ≥ 2.5 mg/mL (5.61 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。
2、请依序添加每种溶剂：10% DMSO→90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.61 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
Solubility: ≥ 2.5 mg/mL (5.61 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。
2、请依序添加每种溶剂：10% DMSO→90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.61 mM); 澄清溶液
此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
靶点：
Tyk2:0.5nM(IC50);JAK2:6nM (IC50);JAK3:8nM(IC50);JAK1:12nM (IC50);Syk:32nM (IC50);MST1:4nM (IC50)
ARK5:4nM (IC50);MLK1:5nM (IC50);FMS: 5nM (IC50);AMPK:6nM (IC50);TBK1:10nM (IC50);MARK1:10nM (IC50)
PAR1B-a TSSK:13nM (IC50);MST2:14nM (IC50);GCK:15nM (IC50); JNK3:18nM (IC50);Rsk2: 20nM (IC50)
Rsk4: 28nM (IC50);CHK1:42nM (IC50);Flt4:51nM (IC50);Flt3: 90nM (IC50);Ret:105nM (IC50); Itk: 194nM (IC50)
ARK5:4nM (IC50);MLK1:5nM (IC50);FMS: 5nM (IC50);AMPK:6nM (IC50);TBK1:10nM (IC50);MARK1:10nM (IC50)
PAR1B-a TSSK:13nM (IC50);MST2:14nM (IC50);GCK:15nM (IC50); JNK3:18nM (IC50);Rsk2: 20nM (IC50)
Rsk4: 28nM (IC50);CHK1:42nM (IC50);Flt4:51nM (IC50);Flt3: 90nM (IC50);Ret:105nM (IC50); Itk: 194nM (IC50)
体外研究：
Cerdulatinib shows inhibitory effect on 60 CLL with IC50 ranging from 0.37 to 10.02 µM. Cerdulatinib induces apoptosis in CLL in association with MCL-1 down-regulation and PARP cleavage. Cerdulatinib (2μM) is able to overcome the support of the microenvironment and induces CLL cell death. Cerdulatinib (250-500 nM) blocks proliferation of ibrutinib-sensitive and ibrutinib-resistant primary CLL cells. Cerdulatinib also blocks proliferation of both ibrutinib-sensitive and ibrutinib-resistant primary CLL cells as well as BTKC481S-transfected cell lines, and blocks BCR and JAK-STAT signaling pathways. Furthermore, inhibition of SYK and JAK by cerdulatinib translates to downstream inhibition of AKT and ERK. Cerdulatinib inhibits the activity of NF-kB pathway. PRT062070 reduces the ability of stimulated B cells to upregulate cell-surface expression of the early activation marker CD69 (IC50=0.11 µM). PRT062070 exhibits differential potency against cytokine JAK/STAT signaling pathways. PRT062070 (1 or 3 µM) induces apoptosis in BCR-signaling competent NHL cell lines. Cerdulatinib demonstrates inhibitory activity against both ABC and GCB subtypes of DLBCL cells. Cerdulatinib also induces apoptosis in both GCB and ABC subtypes of DLBCL cell lines via caspase 3 and PARP cleavage. And cerdulatinib blocks cell cycle in both ABC and GCB subtypes of DLBCL via inhibition of RB phosphorylation and down-regulation of cyclin E. Cerdulatinib induces cell cycle arrest and apoptosis under the condition of BCR stimulation in all DLBCL cell lines. Besides, cerdulatinib blocks JAK/STAT and BCR signaling in both ABC and GCB DLBCL cell lines. Cerdulatinib induces cell death in primary human DLBCL samples. Cerdulatinib inhibits BCR-induced signals in a dose-dependent manner and most strongly between 0.3 to 1 μM. and particularly in IGHV-unmutated samples with greater BCR signaling capacity and response to IL4, or samples expressing higher levels of sIgM, CD49d+, or ZAP70+. Cerdulatinib overcomes anti-IgM, IL4/CD40L, or NLC-mediated protection by preventing upregulation of MCL-1 and BCL-XL; however, BCL-2 expression is unaffected. Furthermore, in samples treated with IL4/CD40L, cerdulatinib synergizes with venetoclax in vitro to induce greater apoptosis than either drug alone.
体内研究：
PRT062070 (0.5 mg/kg) results in a nonstatistically significant trend toward reduced ankle inflammation, whereas significant reductions in inflammation are achieved with the 1.5, 3, and 5 mg/kg doses. PRT062070 also affects anticollagen antibody formation. PRT062070 (15 mg/kg) suppresses upregulation of splenic B-cell surface CD80/86 and CD69, and inhibits BCR signaling and activation in the spleen after oral dosing in mice.
保存条件：
-20°C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献
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