Pacritinib (SB1518)

For research use only. Not for use in humans.

目录号:S8057

Pacritinib (SB1518) Chemical Structure

CAS No. 937272-79-2

Pacritinib (SB1518)是有效的选择性Janus Kinase 2 (JAK2)Fms-Like Tyrosine Kinase-3 (FLT3)抑制剂,无细胞试验中IC50分别为23和22 nM。Phase 3。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 3677.31 现货
RMB 2438.19 现货
RMB 12203.1 现货
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客户使用Selleck生产的Pacritinib (SB1518)发表文献7篇:

客户使用该产品的1个实验数据:

  • Phosphorylation of the CSF-1R targets indicated was examined by immunoblotting

    Clin Cancer Res, 2016, 22(24):6118-6128. Pacritinib (SB1518) purchased from Selleck.

产品安全说明书

JAK抑制剂选择性比较

生物活性

产品描述 Pacritinib (SB1518)是有效的选择性Janus Kinase 2 (JAK2)Fms-Like Tyrosine Kinase-3 (FLT3)抑制剂,无细胞试验中IC50分别为23和22 nM。Phase 3。
特性 双重JAK2/FLT3抑制剂,治疗骨髓纤维化正处于3期临床阶段。
靶点
FLT3 (D835Y) [1]
(Cell-free assay)
JAK2 (V617F) [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
TYK2 [1]
(Cell-free assay)
6 nM 19 nM 22 nM 23 nM 50 nM
体外研究

Pacritinib是野生型JAK2和JAK2V617F的抑制剂(IC 50是19 nM),它高频率存在于MPD患者中。相对于JAK2,Pacritinib对TYK2(IC 50是50 nM)的抑制作用低2倍,对JAK3(IC 50是520 nM)的抑制作用低23倍,对JAK1(IC 50是50 nM)的抑制作用低56倍。Pacritinib有效地渗透细胞调节JAK2的下游信号通路,无论是受体激动剂激活或突变型激活。在JAK2WT- and JAK2V617F-缺少细胞中,Pacritinib诱导细胞凋亡,细胞周期阻滞和抗增殖作用。Pacritinib抑制Karpas 1106P and Ba/F3-JAK2V617F细胞增殖,IC 50分别是348 nM和160 nM。Pacritinib从抑制红细胞和髓系祖细胞来源的内在性菌落生长,IC50分别为63 nM和53 nM。[1] SB1518也抑制FLT3基因及突变FLT3-D835Y(IC50是6 nM)。在FLT3基因内部串联重复(ITD),FLT3-野生型细胞和原发性AML原始细胞中,Pacritinib抑制FLT3磷酸化和下游STAT,MAPK和PI3K信号。 在含FLT3-ITD的MV4-11细胞中,Pacritinib剂量依赖性减少pFLT3,pSTAT5,PERK1/ 2和pAKT,IC50分别为80 nM,40 nM,33 nM和29 nM。Pacritinib处理原代AML细胞3小时剂量依赖性的减少pFLT3,pSTAT3和pSTAT5,IC 50低于0.5 μM。在FLT3突变和FLT3-wt细胞中,Pacritinib诱导细胞凋亡,细胞周期停滞和抗增殖作用。Pacritinib抑制含FLT3-ITD的MV4-11细胞和原代AML细胞增殖,IC50分别为47 nM 和0.19-1.3 nM。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM14 M3PXd2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVS0PEBpenN? Ml\kRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgbIFz[m:{aX7nJGZNXDNvSWTEJI12fGGwdDDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IECuNFc6KM7:TT6= M1jHU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
MCF7 NYrXUW4xSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M4nwTVczKGi{cx?= M{LjZ2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iMD6yPUDPxE1w MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
HL60 NWf2VHJnSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NHX6[3o1QCCqcoO= Mk[2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKTE[wJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMD61NkDPxE1w NYXmZVZTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
KMS-12-BM Mlz1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NE\1[Ys1QCCqcoO= M2\neWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS13TMVEzNUKPIHPlcIx{KGGodHXyJFQ5KGi{czDifUBE\WyuVHn0[ZIuT2yxIHHzd4F6NCCLQ{WwJF0hOC55NTFOwG0v NITvd489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
PC3 NYPvXlRKSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NHHNdZo1QCCqcoO= M3SwUGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMD63O{DPxE1w Mn7wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
Jurkat MnvBRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MUi0PEBpenN? MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEq3cnvheEBk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IECuPFM6KM7:TT6= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
MCF7 NVnRNnFRSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NUX6bJc6PDhiaILz Mlj5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMD64OUDPxE1w MkfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
HCT116 M3X0XWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NX\UVG0{PzJiaILz NEPISlRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE45QCEQvF2u NE\FTHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
Jurkat M2TL[GFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NHyy[5hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFr1dotifCClZXzsd{whUUN3MDC9JFEvODlizszNMi=> Mo[3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
HEL 92.1.7 M3r1UGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVPpcGQxOzZiaILz NXrseYhTSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBJTUxiOUKuNU44KGOnbHzzJIhiemKxcnnu[{BLSUt{IG[2NVdHKG23dHHueEBi\nSncjCzOkBpenNiYomgVJJme3SxQnz1[UBlgWViYnHz[YQh[XO|YYmsJGlEPTBiPTCxMlE4KM7:TT6= MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
OPM2 NUPaRZZ{SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NVHScoRrPDhiaILz NUPqbW0xSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDPVG0zKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyIE2gNU4zOSEQvF2u NH3T[XU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
KHYG NX7UTYJYSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NH3vdWY1QCCqcoO= NX7jXFVjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLTHlIKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyIE2gNU4zPCEQvF2u M1PWZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
KG1 NGK1UmFCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MX20PEBpenN? MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuJMTDj[YxteyCjZoTldkA1QCCqcoOgZpkhS2WubGTpeIVzNUeubzDhd5NigSxiSVO1NEA:KDFwNEig{txONg>? Ml:1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
NKYS NVzlWIRNSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MlOwOFghcHK| NYS3coFSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOT3lUKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyIE2gNU43KM7:TT6= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
HCT116 MV\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NIDFUW41QCCqcoO= M2rwOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyIE2gNU43QSEQvF2u MkDlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
HEL 92.1.7 Mn;1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MlfMOFghcHK| NUPJcWE{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBJTUxiOUKuNU44KGOnbHzzJIhiemKxcnnu[{BLSUt{IG[2NVdHKG23dHHueEBi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFEvPzJ4IN88UU4> MkjWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
HL60 NX3DTGZUSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NIG3R3ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMOlAh[2WubIOsJGlEPTBiPTCxMlc5KM7:TT6= M37ZSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
PC3 M{X4XWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NWLMT4xRPzJiaILz MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOi52MTFOwG0v NYHtRmN1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
MDA-MB-231 MWXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MUW3NkBpenN? NYLYVnBvSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB{LkSzJO69VS5? NUS2R|IyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
TAMH NVTNNlRLSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NIPWZVgzPCCqcoO= MoHMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCWQV3IJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMz62PEDPxE1w MorHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
MOLM14 Mm\2RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NGDST5M1QCCqcoO= NE\G[nlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUG0yPCClZXzsd{Bi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDhd5NigSxiSVO1NEA:KDBwMEe5JO69VS5? NXjVbIx3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVM{QDZpPkK4PVU{Ozh4PD;hQi=>
KMS-12-BM NFXPbIZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NXLEcYJ5PDhiaILz MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuPUz2xNk1DVSClZXzsd{Bi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDhd5NigSxiSVO1NEA:KDBwN{Wg{txONg>? NV20Nm5NRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVM{QDZpPkK4PVU{Ozh4PD;hQi=>
Jurkat M{nPOWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NWfLS4l4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDKeZJs[XRiY3XscJMtKEmFNUCgQUAyNjB7IN88UU4> MoDDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
HEL 92.1.7 NHzXVpNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NH3sR2M{PiCqcoO= NIrPNINCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjFUEA6Oi5zLkegZ4VtdHNiYX\0[ZIhOzZiaILzJIJ6KFC{ZYP0c2JtfWViZInlJIJie2WmIHHzd4F6NCCLQ{WwJF0hOS5zNzFOwG0v M1HNeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUWzN|g3Lz5{OEm1N|M5PjxxYU6=
OPM2 MkniRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NHryS2I1QCCqcoO= MmnyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCRUF2yJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGG|c3H5MEBKSzVyIE2gNU4zOSEQvF2u NY[0[4tLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVM{QDZpPkK4PVU{Ozh4PD;hQi=>
KHYG NVrOUo4xSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NYfyeoRHPDhiaILz M4HxOmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1jZS{Bk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{BtfW2rbnXzZ4VvfCCjc4PhfUwhUUN3MDC9JFEvOjRizszNMi=> M3\WVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUWzN|g3Lz5{OEm1N|M5PjxxYU6=
KG1 MWPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MoHrOFghcHK| MoCxRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNR{GgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO|YYmsJGlEPTBiPTCxMlQ5KM7:TT6= M3;PclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUWzN|g3Lz5{OEm1N|M5PjxxYU6=
NKYS MXXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M{TWTlQ5KGi{cx?= NYjxSVl2SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOT3lUKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHHzd4F6NCCLQ{WwJF0hOS54IN88UU4> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3M{O4Okc,Ojh7NUOzPFY9N2F-
HL60 M37oNWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NHrVZ3BCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMOlAh[2WubIOsJGlEPTBiPTCxMlc5KM7:TT6= MnGyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
AC10 M{L1SWN6fG:2b4jpZ4l1gSCjc4PhfS=> NV;2dldiOjRiaILz MXzDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBR|ExKGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IEK0JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyIE2gNk4xOiEQvF2u M2W4OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUWzN|g3Lz5{OEm1N|M5PjxxYU6=
TAMH NH3vSmxEgXSxdH;4bYNqfHliYYPzZZk> NFP0N3czPCCqcoO= NEjiTotEgXSxdH;4bYNqfHliYXfhbY5{fCCWQV3IJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDJ2IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMz62PEDPxE1w MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3M{O4Okc,Ojh7NUOzPFY9N2F-
KMS-12-BM MWHGeY5kfGmxbjDhd5NigQ>? MmDSNkB2VQ>? M1TSTlMhcHK| NIHvT5VKdmirYnn0bY9vKG:oIFrBT|IhcW5iSVytOk1{fGmvdXzheIVlKGi3bXHuJGtOWy1zMj3CUUBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDTWGFVOyCyaH;zdIhwenmuYYTpc44h[XRiVGm3NFUhemW|aXT1[UBifCB{IIXNJJBz\XS{ZXH0[YQh\m:{IEOgbJJ{KG[xbHzve4VlKGK7IFnMMVYhe3SrbYXsZZRqd25iYomgbY1ufW6xYnzveEBu\XSqb3S= NYD1fIFuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
MOLM14 NXnl[4FKTnWwY4Tpc44h[XO|YYm= M4TKV|AvOSC3TR?= NHvjT4I{KGi{cx?= M1L0VWlvcGmkaYTpc44hd2ZiSlHLNkBqdiCLTD22MZN1cW23bHH0[YQhcHWvYX6gUW9NVTF2IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKFOWQWSzJJBpd3OyaH;yfYxifGmxbjDheEBVYTdyNTDy[ZNq\HWnIHH0JFAvOSC3TTDwdoV1emWjdHXkJIZweiB|IHjyd{Bnd2yub4fl[EBjgSCLTD22JJN1cW23bHH0bY9vKGK7IHntcZVvd2Kub4SgcYV1cG:m Ml7SQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
HEL 92.1.7 MlfmSpVv[3Srb36gZZN{[Xl? MV[xJIhz NWHFSJJSUW6mdXP0bY9vKG:oIFrBT|IhXjZzN1[gcZV1[W62IIDoc5NxcG:{eXzheIlwdiCjdDDZNVAxPy96IILld4llfWW|IHnuJGhGVCB7Mj6xMlch[2WubIOgZYZ1\XJiMTDodkBjgSCrbX31co9jdG:2IH3leIhw\A>? Ml62QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pFLT3 / FLT3 / pSTAT5 / STAT5 / GAPDH; 

PubMed: 31102119     


In vitro activity of pacritinib in various FLT3-ITD+ models. (D) Signaling inhibition with pacritinib in Ba/F3 cells expressing different FLT3 double mutants via Western blot (representative images from two experiments).

p-STAT3Y705 / STAT3 / ACTIN / PARP; 

PubMed: 29253028     


Pacritinib effectively decreases BTIC viability and sphere forming capacity and has on-target activity on phospho-STAT3. (D) Pacritinib had on-target activity as seen by a decrease in the phosphorylation of tyrosine 705 at 3 hours. It also resulted in increased cell death as seen by an increase in the cleaved PARP at 24 hours (representative line BT69 shown).

pSTAT3 Y705 / STAT3 / β-Tubulin; 

PubMed: 29253028     


Pacritinib does not attenuate BTIC sensitivity to TMZ. (E) 1 μM pacritinib dramatically reduced phosphorylation of tyrosine 705 of STAT3 (p-STAT3 Y705) in BT53 at 48 hours. Treatment with 10 μg/mL TMZ resulted in a dramatic increase in p-STAT3 Y705. Combinatorial treatment with pacritinib and TMZ resulted in the abrogation of activated STAT3.

pSTAT3 Y705 / STAT3 / Actin / MAPK / p-AKT S473 / AKT; 

PubMed: 29253028     


Pacritinib inhibits STAT3 with minimal effects on other signaling pathways. Low micromolar concentrations of pacritinib reduced phosphorylation of tyrosine 705 of STAT3 in BT147 and BT53 at 3 hours, but did not affect phosphorylation of p44/42 MAPK or AKT S473. Pacritinib reduced phosphorylation of AKT S473 and p44/42 MAPK at higher concentrations (5 μM and 10 μM).

pFLT3(Y591) / pSTAT5(Y694) / pERK1、2 / pAkt(T308) / β-Actin; 

PubMed: 22829080     


Pacritinib effectively blocks FLT3 signaling in FLT3-ITD (MV4-11, MOLM-13) or FLT3-wt (RS;4-11) cells. (a) MV4-11 cells were treated with pacritinib, JAKi-1 and sunitinib for 3 h as indicated. After lysis, phosphorylation status of FLT3, STAT5, ERK1/2 and Akt were detected by immunoblotting (IB). As a loading control, the same membranes were re-probed with anti-actin antibody.

pFLT3(Y591) / pSTAT5(Y694) / pERK1、2 / pAkt(T308) / β-Actin; 

PubMed: 22829080     


Pacritinib effectively blocks FLT3 signaling in FLT3-ITD (MV4-11, MOLM-13) or FLT3-wt (RS;4-11) cells. As a loading control, the same membranes were re-probed with anti-actin antibody. (b) MOLM-13 and (c) RS4;11 cells were pre-treated with pacritinib for 3 h and stimulated for 3 min with 10 ng/ml FLT3 ligand as indicated. After lysis, the phosphorylation status of FLT3 and total actin were detected by IB.

31102119 29253028 22829080
Growth inhibition assay
Cell viability; 

PubMed: 29235481     


Effects of UC-514321 in treating AMLs. b–e Effects of NSC-370284, UC-514321, and other JAK/STAT pathway inhibitors, i.e., Pacritinib, KW-2449, Stattic and sc-355979, on the viability of AML cell lines MONOMAC-6 (b), THP-1 (c), KASUMI1 (d), and NB4 (e). Cells were treated with drugs at indicated doses. Cell viability was detected by MTS 48 h post treatment. Error bar indicates SD of triplicate experiments.

29235481
IHC
HE staining of liver sections; 

PubMed: 29785143     


Representative micrography of H&E-stained liver sections on day of death. H&E (hematoxylin and eosin).

HE staining of skin grafts; 

PubMed: 29382747     


(C) Histologic representations of the skin grafts uniformly harvested on day +21 demonstrate that pacritinib reduces lymphocytic infiltration (^) and severe basal vacuolar changes of the graft, such as the subepidermal blister (#). Low power at 6×, high-power Inset at 20×. (Scale bar, 400 µm.)

p-STAT3 / Ki-67 / mCD31 / VEGF-A / Bcl-2; 

PubMed: 32929154     


Combined treatment with JAK2 and SMO inhibitors synergize to reduce angiogenesis, tumor cell proliferation, and tumoral STAT3 activation of TNBC in vivo. (B) Representative IHC images of Bcl-2, VEGF-A, mCD31, Ki-67, and p-STAT3 (Y705) of treated MDA-231 MFP xenografts. Images were taken under 20X magnification. Arrows point to examples of positive staining.

29785143 29382747 32929154
Immunofluorescence
Phalloidin; 

PubMed: 27334834     


Pacritinib inhibits nurse-like cell viability. (C) NLC were generated from CLL patient PBMC and treated with ruxolitinib (5 μM), fedratinib (5 μM), pacritinib (1 μM) or vehicle control (DMSO). NLC were visualized by fluorescent microscopy 24 hours later after phalloidin and DAPI staining.

TUNEL; 

PubMed: 32929154     


(H) Representative images of TUNEL-positive staining of mammary fat pad xenografts from each treatment group. TUNEL, DAPI, and TUNEL-DAPI merged. Images were taken under 10X magnification. For all analyses, at least 5 fields were quantified per tumor section (N=4–5 tumors/group).

27334834 32929154
体内研究 Pacritinib(150毫克/千克)口服q.d.到JAK2 V617F相关移植瘤模型中,可显著改善脾肿大和肝的症状,使60%脾脏重量和92%肝脏重量的正常化,无显著体重减轻或任何血液学毒性,包括血小板减少症和贫血。 Pacritinib诱导剂量依赖性的抑制了JAK2V617F依赖性的SET-2异种移植物的生长(75毫克/千克时为40%和150毫克/千克时为61%)。[1] Pacritinib对 FLT3-ITD息MV4-11异种移植模型是有效的。 Pacritinib治疗,每日一次,连续21天,诱导了剂量依赖性的肿瘤生长抑制(25毫克/千克时为38%,50毫克/千克时为92%,100毫克/千克时为121%)。在50和100毫克/公斤/天组分别观察到3/10和8/8只小鼠肿瘤完全消退。[2]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

激酶活性检测:

所有测定均在384孔白色微量滴定板中进行。化合物4-倍系列稀释8级,从10μM开始。反应混合物由25 μL的测定缓冲液(50 mM HEPES pH值为7.5 ,10mM氯化镁,5 mM氯化锰,1 mM DTT, 0.1 mM的钒酸钠,5 mM的β -甘油磷酸)。对FLT3的测定中,反应含有2.0微克/毫升的FLT3酶,5 μM聚(谷氨酸,酪氨酸)底物和4 μM ATP。对于JAK1测定中,反应含有2.5微克/毫升JAK1酶,10μM聚(谷氨酸,丙氨酸,酪氨酸)底物和1.0 μM ATP。对于JAK2测定中,反应物含有0.35微克/毫升的JAK2酶,10 μM聚(谷氨酸,丙氨酸,酪氨酸),衬底和0.15 μM ATP。对于JAK3测定中,反应物含有3.5微克/毫升的JAK3酶,10μM聚(谷氨酸,丙氨酸,酪氨酸)底物和6.0 μM的ATP。对TYK2测定中,反应物含有2.5微克/毫升的TYK2酶,10μM聚(谷氨酸,丙氨酸,酪氨酸)底物和0.15 μM ATP。反应在加入13 μL PKLight®检测试剂之前在室温温育2小时。温育10分钟之后读取在多标记平板读数器读取发光信号。
细胞实验:[1]
- 合并
  • Cell lines: Karpas 1106P细胞
  • Concentrations: ~10 μM
  • Incubation Time: 2 天
  • Method: 细胞按30〜50%密度接种在96孔板中,并用不同浓度的化合物(一式三份)处理48小时。细胞活力使用CellTiter-格洛测定检测。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 人巨核细胞白血病移植SET-2
  • Dosages: 150 mg/kg
  • Administration: 口服灌胃
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 11 mg/mL warmed (23.27 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 472.58
化学式

C28H32N4O3

CAS号 937272-79-2
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

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
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Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04520269 Recruiting Drug: Pacritinib Breast Cancer National University Hospital Singapore July 13 2020 Phase 1|Phase 2
NCT03165734 Recruiting Drug: Pacritinib|Drug: Physician''s Choice medications Primary Myelofibrosis|Post-polycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis CTI BioPharma|PSI CRO June 26 2017 Phase 3
NCT02677948 Withdrawn Drug: Pacritinib|Drug: Ibrutinib Chronic Lymphocytic Leukemia|Lymphoma Small Lymphocytic University of Michigan Rogel Cancer Center October 2016 Phase 1|Phase 2
NCT02584777 Withdrawn Biological: Pacritinib Primary Myelofibrosis Baxalta now part of Shire|CTI BioPharma|Takeda November 30 2015 Phase 2
NCT02765724 Completed Drug: Pacritinib Myelofibrosis CTI BioPharma|SGS S.A. January 2015 Phase 1

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操作手册

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JAK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID