Pacritinib (SB1518)

目录号:S8057

仅限科研使用

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。

Pacritinib (SB1518) Chemical Structure

CAS: 937272-79-2

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
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Pacritinib (SB1518)发表文献9篇:

客户使用该产品的1个实验数据:

产品安全说明书

JAK抑制剂选择性比较

相关JAK产品

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)
点击更多
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 M2DpPGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVKzOYhTPDhiaILz MoP5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPT1zNNVQh[2WubIOgbIFz[m:{aX7nJGZNXDNvSWTEJI12fGGwdDDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IECuNFc6KM7:TT6= M3XOSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
MCF7 MlS1RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M{ewO|czKGi{cx?= MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDBwMkmg{txONg>? NXf0fItGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
HL60 NHLBZ5hCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MlrJOFghcHK| M2W0V2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IECuOVIh|ryPLh?= M3vqZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
KMS-12-BM Mn3uRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXfWT5YyPDhiaILz NXqwN2pJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLUXMuOTJvQl2gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOnbHzUbZRmei2JbH:gZZN{[XluIFnDOVAhRSByLke1JO69VS5? M{K4[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
PC3 M2rNOGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXHqN3hnPDhiaILz NVziWYRnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDQR|Mh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCwMlc4KM7:TT6= MojoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
Jurkat MlW3RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MWG0PEBpenN? NHWxW2RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFr1dotifCClZXzsd{Bi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFAvQDN7IN88UU4> NGfaVFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
MCF7 Ml\2RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3j1ZlQ5KGi{cx?= NIHKcYxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCwMlg2KM7:TT6= MoC4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
HCT116 NWXrZY5kSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= Mn\GO|IhcHK| NGDkT4pCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE45QCEQvF2u NE\6O449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
Jurkat NEO2S4lCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEq3cnvheEBk\WyuczygTWM2OCB;IEGuNFkh|ryPLh?= NXmybmpXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
HEL 92.1.7 M2m0d2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NIKyfIs{PiCqcoO= NYO2d2NESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBJTUxiOUKuNU44KGOnbHzzJIhiemKxcnnu[{BLSUt{IG[2NVdHKG23dHHueEBi\nSncjCzOkBpenNiYomgVJJme3SxQnz1[UBlgWViYnHz[YQh[XO|YYmsJGlEPTBiPTCxMlE4KM7:TT6= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
OPM2 NGDGbm5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NUHPTWx3PDhiaILz MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:STUKgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOnbHzUbZRmei2JbH:gZZN{[XluIFnDOVAhRSBzLkKxJO69VS5? NVvld4pTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
KHYG Mm\SRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MWq0PEBpenN? NH36e3dCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvIXWch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCxMlI1KM7:TT6= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
KG1 MUHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NUPrbllHPDhiaILz MXrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuJMTDj[YxteyCjZoTldkA1QCCqcoOgZpkhS2WubGTpeIVzNUeubzDhd5NigSxiSVO1NEA:KDFwNEig{txONg>? NVfjSZRLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
NKYS MYfBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MX60PEBpenN? NGjrVGRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7LXXMh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCxMlYh|ryPLh?= MoXIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
HCT116 Ml\4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M325SFQ5KGi{cx?= MUHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IEGuOlkh|ryPLh?= NFPzcI09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
HEL 92.1.7 MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NGL1Rog1QCCqcoO= NVHPO4hFSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBJTUxiOUKuNU44KGOnbHzzJIhiemKxcnnu[{BLSUt{IG[2NVdHKG23dHHueEBi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFEvPzJ4IN88UU4> NIHS[5Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
HL60 M3fT[2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNuIFnDOVAhRSBzLke4JO69VS5? M4DNPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
PC3 NGLmSJVCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mo\LO|IhcHK| MV\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOi52MTFOwG0v M1nUSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
MDA-MB-231 M3jlemFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NVjJTpN[PzJiaILz MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk0zOzFiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFIvPDNizszNMi=> NWL1NZZ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
TAMH M1y5R2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 MkC3NlQhcHK| NIn4[2pCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JI1wfXOnIGTBUWgh[2WubIOgZYZ1\XJiMkSgbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCzMlY5KM7:TT6= M4XCXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
MOLM14 MXnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVO0PEBpenN? NYTFcG83SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTRiY3XscJMh[W[2ZYKgOFghcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZZN{[XluIFnDOVAhRSByLkC3PUDPxE1w MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3M{O4Okc,Ojh7NUOzPFY9N2F-
KMS-12-BM NXfURWlWSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NYfmSHlRPDhiaILz MmHCRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNTWOtNVIuSk1iY3XscJMh[W[2ZYKgOFghcHK|IHL5JGNmdGyWaYTldk1IdG9ibIXtbY5me2OnboSgZZN{[XluIFnDOVAhRSByLke1JO69VS5? NIHWZpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1N|M5Pid-Mki5OVM{QDZ:L3G+
Jurkat NFTxWFdCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4Wxb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSoXyb4F1KGOnbHzzMEBKSzVyIE2gNU4xQSEQvF2u NGr2VZI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1N|M5Pid-Mki5OVM{QDZ:L3G+
HEL 92.1.7 NGf2XHZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NX3iTYZwOzZiaILz M2DUZWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFXMJFkzNjFwNzDj[YxteyCjZoTldkA{PiCqcoOgZpkhWHKnc4TvRox2\SCmeXWgZoF{\WRiYYPzZZktKEmFNUCgQUAyNjF5IN88UU4> NXPEVHNoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVM{QDZpPkK4PVU{Ozh4PD;hQi=>
OPM2 MofPRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M{nSSFQ5KGi{cx?= NFfTW4VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;QUVIh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiYYPzZZktKEmFNUCgQUAyNjJzIN88UU4> MoTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
KHYG NE\JRlhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NIWwb|k1QCCqcoO= NEDTbG1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvIXWch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncj3HcI8hdHWvaX7ld4NmdnRiYYPzZZktKEmFNUCgQUAyNjJ2IN88UU4> MkTrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
KG1 M1v1XGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXy0PEBpenN? M2fZUmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1exJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIx2dWmwZYPj[Y51KGG|c3H5MEBKSzVyIE2gNU41QCEQvF2u NYXFOoZYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5OVM{QDZpPkK4PVU{Ozh4PD;hQi=>
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HL60 M4\oSmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M{foO2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczygTWM2OCB;IEGuO|gh|ryPLh?= MoHqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
AC10 NIDkOZpEgXSxdH;4bYNqfHliYYPzZZk> M322blI1KGi{cx?= M2\ONmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGFEOTBiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgNlQhcHK|IHL5JGNmdGyWaYTldk1IdG9iYYPzZZktKEmFNUCgQUAzNjB{IN88UU4> Mlu3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
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MOLM14 NUjYNGRnTnWwY4Tpc44h[XO|YYm= MX[wMlEhfU1? NF36O3k{KGi{cx?= NHn1PFZKdmirYnn0bY9vKG:oIFrBT|IhcW5iSVytOk1{fGmvdXzheIVlKGi3bXHuJG1QVE1zNDDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhXFl5MEWgdoV{cWS3ZTDheEAxNjFidV2gdJJmfHKnYYTl[EBnd3JiMzDodpMh\m:ubH;3[YQh[nliSVytOkB{fGmvdXzheIlwdiCkeTDpcY12dm:kbH;0JI1mfGixZB?= M3:3R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
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Assay
Methods Test Index PMID
Western blot pFLT3 / FLT3 / pSTAT5 / STAT5 / GAPDH p-STAT3Y705 / STAT3 / ACTIN / PARP pSTAT3 Y705 / STAT3 / β-Tubulin pSTAT3 Y705 / STAT3 / Actin / MAPK / p-AKT S473 / AKT pFLT3(Y591) / pSTAT5(Y694) / pERK1、2 / pAkt(T308) / β-Actin pFLT3(Y591) / pSTAT5(Y694) / pERK1、2 / pAkt(T308) / β-Actin 31102119 29253028 22829080
Growth inhibition assay Cell viability 29235481
IHC HE staining of liver sections HE staining of skin grafts p-STAT3 / Ki-67 / mCD31 / VEGF-A / Bcl-2 29785143 29382747 32929154
Immunofluorescence Phalloidin TUNEL 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]
  • 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]
  • 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。
动物实验:[1]
  • Animal Models: 人巨核细胞白血病移植SET-2
  • Dosages: 150 mg/kg
  • Administration: 口服灌胃

溶解度(25°C)

体外

* 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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

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,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法: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 ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意: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。

摩尔浓度计算器

质量 浓度 体积 分子量

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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