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CAS No.: 1198300-79-6

Cerdulatinib Catalog No. CSN13905

Synonyms: PRT062070;PRT2070

Cerdulatinib is a multiple tyrosine kinase inhibitor with IC50 values of 12 nM/6 nM/8 nM and 0.5 nM, for JAK1/JAK2/JAK3 and TYK2, also shows potency against MST1, ARK5, MLK1, Fms. Syk, etc. with IC50 values ranging in 4-51 nM.

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生物活性

描述The JAK/STAT pathway forms a critical node affecting multiple signaling pathways in both the innate and adaptive immune responses. JAK family members include Janus kinases 1, 2, and 3 (JAK1, JAK2, and JAK3, respectively) and tyrosine kinase 2 (TYK2). JAK1 and JAK2 and TYK2 are broadly activated by different cytokines across cell types, while JAK3 is limited to primarily hematopoietic cells. Cerdulatinib/PRT-062070 is an orally active nonspecific kinase inhibitor with an IC₅₀ of 0.5, 12, 6, or 8 nM for TYK2, JAK1, JAK2, or JAK3, respectively. At the cellular level, cerdulatinib demonstrates specificity towards JAK1/JAK3 and TYK2, but not JAK2-mediated responses and it is currently in phase 1/2A clinical trials for CLL (chronic lymphocytic leukemia) as well as other B-cell Non Hodgkin lymphomas, with first in man clinical trial data and therapeutic responses in patients resistant to ibrutinib already reported. The specificity of cerdulatinib was also demonstrated by its lack of inhibition of T cell receptor signaling or protein kinase C signaling in whole blood^[3]. On a tissue microarray of 62 primary DLBCL (large B-cell lymphoma) tumors with 58% expressed either phosphorylated SYK or STAT3 or both. Cerdulatinib induced DLBCL cells apoptosis which was associated with caspase-3 and PARP cleavage with IC₅₀ of 32 nM and 12 nM for SYK and JAK1^[4]. PBMCs from CLL patients were treated with cerdulatinib ranging from 0-1μM. Cerdulatinib induced apoptosis of CLL cells in a time- and concentration-dependent manner, and particularly in IGHV unmutated samples with greater BCR-signaling capacity and response to IL-4, which showed that Cerdulatinib is a promising therapeutic for the treatment of CLL either alone or in combination with venetoclax^[5].
作用机制The functional groups that interact with Leu377, Gly378, and Val385 in the G-loop and the nearby region in SYK (Spleen tyrosine kinase) can bind to the enzyme pocket.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01994382	Follicular Lymphoma (FL/Indole... more >>nt NHL) Aggressive NHL (a NHL) Chronic Lymphocytic Leukemia (CLL) / Small Lymphocytic Lymphoma (SLL) T-cell Lymphoma (PTCL and CTCL) B-cell Non Hodgkin Lymphoma (NHL) Collapse <<	Phase 1 Phase 2	Recruiting	December 2019	-

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2445 mL
- 11.2224 mL
- 22.4447 mL
- 5 mM
- 0.4489 mL
- 2.2445 mL
- 4.4889 mL
- 10 mM
- 0.2244 mL
- 1.1222 mL
- 2.2445 mL

技术信息

CAS号

1198300-79-6

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H27N7O3S

运输

蓝冰

分子量

445.54

别名

PRT062070;PRT2070

溶解度

DMSO	50.0 mg/mL (112.2 mM)

动物实验配方

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