Cerdulatinib hydrochloride
(Synonyms: CERDULATINIB盐酸盐,PRT062070 hydrochloride; PRT2070 hydrochloride) 目录号 : GC60687A dual inhibitor of Syk and JAKs
Cas No.:1369761-01-2
Sample solution is provided at 25 µL, 10mM.
Cerdulatinib is a dual inhibitor of spleen tyrosine kinase (Syk) and Janus kinases (JAK; IC50s = 32, 12, 6, 8, and 0.5 nM for Syk, JAK1, JAK2, JAK3, and TYK2, respectively) and also exhibits nanomolar inhibition of other kinases.1 Syk is involved in the B cell receptor (BCR) pathway, and cerdulatinib inhibits downstream Syk-mediated signaling of ERK Y204 phosphorylation (IC50 = 0.5 μM), upregulates cell surface expression of CD69 (IC50 = 0.11 μM), and inhibits FcεRI-mediated basophil degranulation (IC50 = 0.12 μM).1 JAK is involved in JAK-STAT regulation of cytokine receptors. Cerdulatinib inhibits STAT3, STAT5, and STAT6 phosphorylation by interleukin-activated JAK1/3 with IC50 values ranging from 0.16 to 1 μM.1 Cerdulatinib disrupts JAK1/3-mediated signaling more selectively than JAK2 signaling (IC50 > 4 μM).1 Cerdulatinib displays potent antitumor activity against ABC and GCB types of diffuse large B cell lymphoma (DLBCL) by inducing apoptosis via caspase-2 and poly(ADP-ribose) polymerase (PARP) cleavage.2 Cerdulatinib exhibits IC50 values ranging from 0.05 to 2.1 μM against a panel of DLBCL tumor cell lines.2
1.Coffey, G., Betz, A., DeGuzman, F., et al.The novel kinase inhibitor PRT062070 (Cerdulatinib) demonstrates efficacy in models of autoimmunity and B-cell cancerJ. Pharmacol. Exp. Ther.351(3)538-548(2014) 2.Ma, J., Xing, W., Coffey, G., et al.Cerdulatinib, a novel dual SYK/JAK kinase inhibitor, has broad anti-tumor activity in both ABC and GCB types of diffuse large B cell lymphomaOncotarget6(41)43881-43896(2015)
Cas No. | 1369761-01-2 | SDF | |
别名 | CERDULATINIB盐酸盐,PRT062070 hydrochloride; PRT2070 hydrochloride | ||
Canonical SMILES | O=S(N(CC1)CCN1C2=CC=C(NC3=NC=C(C(N)=O)C(NC4CC4)=N3)C=C2)(CC)=O.Cl | ||
分子式 | C20H28ClN7O3S | 分子量 | 482 |
溶解度 | 储存条件 | Store at -20°C | |
General tips | 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。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.0747 mL | 10.3734 mL | 20.7469 mL |
5 mM | 0.4149 mL | 2.0747 mL | 4.1494 mL |
10 mM | 0.2075 mL | 1.0373 mL | 2.0747 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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