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Cerdulatinib hydrochloride Sale

(Synonyms: CERDULATINIB盐酸盐,PRT062070 hydrochloride; PRT2070 hydrochloride) 目录号 : GC60687

A dual inhibitor of Syk and JAKs

Cerdulatinib hydrochloride Chemical Structure

Cas No.:1369761-01-2

规格 价格 库存 购买数量
5mg
¥720.00
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10mg
¥1,080.00
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50mg
¥3,240.00
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100mg
¥5,580.00
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Sample solution is provided at 25 µL, 10mM.

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Description

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)

化学性质

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
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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。
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。

溶解性数据

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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
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