Pacritinib (SB1518)

Catalog No.S8057

For research use only.

Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.

Pacritinib (SB1518) Chemical Structure

CAS No. 937272-79-2

Selleck's Pacritinib (SB1518) has been cited by 11 Publications

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Biological Activity

Description Pacritinib (SB1518) is a potent and selective inhibitor of Janus Kinase 2 (JAK2) and Fms-Like Tyrosine Kinase-3 (FLT3) with IC50s of 23 and 22 nM in cell-free assays, respectively. Phase 3.
Features Dual JAK2/FLT3 inhibitor that has progressed to Phase III clinical trials for treatment of Myelofibrosis.
Targets
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)
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6 nM 19 nM 22 nM 23 nM 50 nM
In vitro

Pacritinib is a potent inhibitor of both wild-type JAK2 and JAK2V617F mutant (IC50= 19 nM) that is present in high frequencies among patients with MPD. Relative to JAK2, Pacritinib is two-fold less potent against TYK2 (IC50= 50 nM), 23-fold less potent against JAK3 (IC50= 520 nM) and 56-fold less potent against JAK1 (IC50= 1280 nM). Pacritinib effectively permeates cells to modulate signaling pathways downstream of JAK2, whether agonist activated or mutationally activated. Pacritinib induces apoptosis, cell cycle arrest and antiproliferative effects in JAK2WT- and JAK2V617F-dependent cells. Pacritinib inhibits cell proliferation of Karpas 1106P and Ba/F3-JAK2V617F with IC50 of 348 and 160 nM, respectively. Pacritinib inhibits endogenous colony growth derived from erythroid and myeloid progenitors with IC50 of 63 and 53 nM , respectively. [1] SB1518 also inhibits FLT3 and its mutant FLT3-D835Y(IC50= 6 nM ). Pacritinib inhibits FLT3 phosphorylation and downstream STAT, MAPK and PI3K signaling in FLT3-internal-tandem duplication (ITD), FLT3-wt cells and primary AML blast cells. Pacritinib treatment leads to a dose-dependent decrease of pFLT3, pSTAT5, pERK1/2 and pAkt in FLT3-ITD harboring MV4-11 cells with IC50 of 80, 40, 33 and 29 nM , respectively. Treatment of the primary AML blast cells with Pacritinib for 3 h leads to a dose-dependent decrease of pFLT3, pSTAT3 and pSTAT5 with an IC50 below 0.5 μM. Pacritinib induces apoptosis, cell cycle arrest and anti-proliferative effects in FLT3-mutant and FLT3-wt cells. Pacritinib inhibits cell proliferation of FLT3-ITD-harboring cells MV4-11 and primary AML blast cells with IC50s of 47 nM and 0.19-1.3 μM, respectively. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MOLM14 M2\PN2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 M37XSlQ5KGi{cx?= NVK2[GFESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNU2xOOTRiY3XscJMhcGG{Yn;ybY5oKE[OVEOtTXRFKG23dHHueEBi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFAvODd7IN88UU4> NELGeHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
MCF7 NEHHRmZCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NIKyN|A4OiCqcoO= MnnMRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSByLkK5JO69VS5? MlqzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
HL60 M3TSSmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NXriXYVJPDhiaILz M3rPNGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IECuOVIh|ryPLh?= M{XEVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
KMS-12-BM NGXnOJNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MXm0PEBpenN? NUDSOm81SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLUXMuOTJvQl2gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOnbHzUbZRmei2JbH:gZZN{[XluIFnDOVAhRSByLke1JO69VS5? NGrrSY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
PC3 Mne4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NXHWZ2FnPDhiaILz M1LMdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUFOzJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMD63O{DPxE1w MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
Jurkat M1LLPGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MmrOOFghcHK| MY\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEq3cnvheEBk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IECuPFM6KM7:TT6= M3vqcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
MCF7 MV\BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MmTPOFghcHK| NH\CRnBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCwMlg2KM7:TT6= NWXHXIlRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
HCT116 NGj1OYNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MnOxO|IhcHK| NH\aR3RCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNE45QCEQvF2u MoLqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
Jurkat NEjhZYNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NVPyZlV5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDKeZJs[XRiY3XscJMtKEmFNUCgQUAyNjB7IN88UU4> M1zXZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
HEL 92.1.7 MmH4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M2LKT|M3KGi{cx?= M2\NfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgTGVNKDl{LkGuO{Bk\WyuczDoZZJjd3KrbnegTmFMOiCYNkG3SkBufXSjboSgZYZ1\XJiM{[gbJJ{KGK7IGDy[ZN1d0KudXWg[JlmKGKjc3XkJIF{e2G7LDDJR|UxKD1iMT6xO{DPxE1w NXq3[lU3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
OPM2 MoPWRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NYTPVHRSPDhiaILz NFP1bFZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;QUVIh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IFPlcIxVcXSncj3HcI8h[XO|YYmsJGlEPTBiPTCxMlIyKM7:TT6= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
KHYG NH\NSYNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MW[0PEBpenN? M1LsW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1jZS{Bk\WyuczDh[pRmeiB2ODDodpMh[nliQ3XscHRqfGW{LVfsc{Bie3OjeTygTWM2OCB;IEGuNlQh|ryPLh?= M2SySlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
KG1 NHHvUo1CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4\Kd|Q5KGi{cx?= MVjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuJMTDj[YxteyCjZoTldkA1QCCqcoOgZpkhS2WubGTpeIVzNUeubzDhd5NigSxiSVO1NEA:KDFwNEig{txONg>? MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
NKYS M2TXXGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MWm0PEBpenN? MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6NWWOgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOnbHzUbZRmei2JbH:gZZN{[XluIFnDOVAhRSBzLk[g{txONg>? NV31[204RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke1OFE{PTdpPkK3OVQyOzV5PD;hQi=>
HCT116 MVTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MXW0PEBpenN? NF6yWG9CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCjc4PhfUwhUUN3MDC9JFEvPjlizszNMi=> M{jHNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
HEL 92.1.7 NF:zUG5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NGO4Woc1QCCqcoO= NFGxb|VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JGhGVCB7Mj6xMlch[2WubIOgbIFz[m:{aX7nJGpCUzJiVk[xO2YhdXW2YX70JIFnfGW{IES4JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGG|c3H5MEBKSzVyIE2gNU44OjZizszNMi=> Mm\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
HL60 MYLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MWTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNuIFnDOVAhRSBzLke4JO69VS5? NEfnRYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
PC3 M2nIeGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M{m4TlczKGi{cx?= MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFCFMzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOi52MTFOwG0v M2rDflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5NUSxN|U4Lz5{N{W0NVM2PzxxYU6=
MDA-MB-231 NVjyT3huSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3TLSlczKGi{cx?= NHvndmFCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDJwNEOg{txONg>? NGXpPHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{W0NVM2Pyd-Mke1OFE{PTd:L3G+
TAMH MVLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MnmyNlQhcHK| MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKFSDTVigZ4VtdHNiYX\0[ZIhOjRiaILzJIJ6KEOnbHzUbZRmei2JbH:gZZN{[XluIFnDOVAhRSB|Lk[4JO69VS5? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
MOLM14 MUTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NVPUUoxSPDhiaILz NGjBNIZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3PUG0yPCClZXzsd{Bi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDhd5NigSxiSVO1NEA:KDBwMEe5JO69VS5? Ml;NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
KMS-12-BM Ml;CRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MmThOFghcHK| MV;BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuPUz2xNk1DVSClZXzsd{Bi\nSncjC0PEBpenNiYomgR4VtdFSrdHXyMWdtdyCudX3pcoV{[2WwdDDhd5NigSxiSVO1NEA:KDBwN{Wg{txONg>? MnTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
Jurkat M3jGVmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NI\4[|VCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFr1dotifCClZXzsd{whUUN3MDC9JFEvODlizszNMi=> NFuyfmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1N|M5Pid-Mki5OVM{QDZ:L3G+
HEL 92.1.7 NWLBNHJ4SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M{nmR|M3KGi{cx?= M1jiUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFXMJFkzNjFwNzDj[YxteyCjZoTldkA{PiCqcoOgZpkhWHKnc4TvRox2\SCmeXWgZoF{\WRiYYPzZZktKEmFNUCgQUAyNjF5IN88UU4> MmfnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7NUOzPFYoRjJ6OUWzN|g3RC:jPh?=
OPM2 NHPGdJhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4nYRlQ5KGi{cx?= MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:STUKgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO|YYmsJGlEPTBiPTCxMlIyKM7:TT6= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3M{O4Okc,Ojh7NUOzPFY9N2F-
KHYG M2ntTGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVu0PEBpenN? MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEuKWVegZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO|YYmsJGlEPTBiPTCxMlI1KM7:TT6= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3M{O4Okc,Ojh7NUOzPFY9N2F-
KG1 M1LFRWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MmnhOFghcHK| Mn7YRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNR{GgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KEOnbHzUbZRmei2JbH:gcJVucW6nc3PlcpQh[XO|YYmsJGlEPTBiPTCxMlQ5KM7:TT6= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDl3M{O4Okc,Ojh7NUOzPFY9N2F-
NKYS NFjSVGRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MUC0PEBpenN? NVryNZl5SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOT3lUKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDD[YxtXGm2ZYKtS4xwKGy3bXnu[ZNk\W62IHHzd4F6NCCLQ{WwJF0hOS54IN88UU4> M1rmN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6OUWzN|g3Lz5{OEm1N|M5PjxxYU6=
HL60 NU\ieXJ4SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3[yT2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczygTWM2OCB;IEGuO|gh|ryPLh?= NIfEPIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1N|M5Pid-Mki5OVM{QDZ:L3G+
AC10 MVrDfZRwfG:6aXPpeJkh[XO|YYm= M4W4RVI1KGi{cx?= NIrLdmFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCSzFyIHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwhfmmjYnnsbZR6KGGodHXyJFI1KGi{czDifUBE\WyuVHn0[ZIuT2yxIHHzd4F6NCCLQ{WwJF0hOi5yMjFOwG0v NEnZbJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1N|M5Pid-Mki5OVM{QDZ:L3G+
TAMH MoTPR5l1d3SxeHnjbZR6KGG|c3H5 M121e|I1KGi{cx?= NEX2U5lEgXSxdH;4bYNqfHliYXfhbY5{fCCWQV3IJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDJ2IHjyd{BjgSCFZXzsWIl1\XJvR3zvJIF{e2G7LDDJR|UxKD1iMz62PEDPxE1w NHzuWlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEm1N|M5Pid-Mki5OVM{QDZ:L3G+
KMS-12-BM M4CxOGZ2dmO2aX;uJIF{e2G7 NGXSfngzKHWP NXPzV|EyOyCqcoO= NEKxNXpKdmirYnn0bY9vKG:oIFrBT|IhcW5iSVytOk1{fGmvdXzheIVlKGi3bXHuJGtOWy1zMj3CUUBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDTWGFVOyCyaH;zdIhwenmuYYTpc44h[XRiVGm3NFUhemW|aXT1[UBifCB{IIXNJJBz\XS{ZXH0[YQh\m:{IEOgbJJ{KG[xbHzve4VlKGK7IFnMMVYhe3SrbYXsZZRqd25iYomgbY1ufW6xYnzveEBu\XSqb3S= MnqxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
MOLM14 NELBVopHfW6ldHnvckBie3OjeR?= MmfmNE4yKHWP NGrjUWw{KGi{cx?= NF;ofGpKdmirYnn0bY9vKG:oIFrBT|IhcW5iSVytOk1{fGmvdXzheIVlKGi3bXHuJG1QVE1zNDDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCVVFHUN{BxcG:|cHjvdplt[XSrb36gZZQhXFl5MEWgdoV{cWS3ZTDheEAxNjFidV2gdJJmfHKnYYTl[EBnd3JiMzDodpMh\m:ubH;3[YQh[nliSVytOkB{fGmvdXzheIlwdiCkeTDpcY12dm:kbH;0JI1mfGixZB?= MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzV2MUO1O{c,Ojd3NEGzOVc9N2F-
HEL 92.1.7 NV;5XpFHTnWwY4Tpc44h[XO|YYm= Mm\DNUBpeg>? MUjJcoR2[3Srb36gc4YhUkGNMjDWOlE4TiCvdYThcpQheGixc4Doc5J6dGG2aX;uJIF1KFlzMEC3M|ghemW|aXT1[ZMhcW5iSFXMJFkzNjFwNzDj[YxteyCjZoTldkAyKGi{IHL5JIludXWwb3Lsc5QhdWW2aH;k MmW1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd3NEGzOVcoRjJ5NUSxN|U4RC:jPh?=
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
In vivo Pacritinib administrated at 150 mg/kg p.o. q.d. to JAK2V617F-dependent xenograft model, significantly ameliorates splenomegaly and hepatomegaly symptoms, with 60% normalization of spleen weight and 92% normalization of liver weight and is well tolerated without significant weight loss or any hematological toxicities, including thrombocytopenia and anemia. Pacritinib induces dose-dependent inhibition of tumor growth of JAK2V617F-dependent SET-2 xenograft model (40% for 75 mg/kg and 61% for 150 mg/kg). [1] Pacritinib is efficacious in FLT3-ITD-bearing MV4-11 xenograft models. Pacritinib treated once daily for 21 consecutive days, induces dose-dependent inhibition of tumor growth (38% for 25 mg/kg, 92% for 50 mg/kg and 121% for 100 mg/kg). Complete regression is observed in 3/10 and 8/8 mice for the 50 and 100 mg/kg/day groups, respectively. [2]

Protocol (from reference)

Kinase Assay:[1]
  • kinase activity assays:

    All assays are carried out in 384-well white microtiter plates. Compounds are 4-fold serially diluted in 8 steps, starting from 10 μM. The reaction mixture consisted of 25 μL assay buffer (50 mM HEPES pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 1 mM DTT, 0.1 mM Na3VO4, 5 mM β-glycerol phosphate). For FLT3 assays, the reaction contains 2.0 μg/mL FLT3 enzyme, 5 μM of poly(Glu,Tyr) substrate and 4 μM of ATP. For JAK1 assays, the reaction contains 2.5 μg/mL of JAK1 enzyme, 10 μM of poly(Glu,Ala,Tyr) substrate and 1.0 μM of ATP. For JAK2 assays, the reaction contained 0.35 μg/mL of JAK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. For JAK3 assays, the reaction contained 3.5 μg/mL of JAK3 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 6.0 μM of ATP. For TYK2 assays, the reaction contained 2.5 μg/mL of TYK2 enzyme, 10 μM of poly (Glu,Ala,Tyr) substrate and 0.15 μM of ATP. The reaction is incubated at room temperature for 2 h prior to addition of 13 μL PKLight® detection reagent. After 10 min incubation luminescent signals are read on a multi-label plate reader.

Cell Research:[1]
  • Cell lines: Karpas 1106P cells
  • Concentrations: ~10 μM
  • Incubation Time: 2 days
  • Method: Cells are seeded at 30-50% confluency in 96-well plates and are treated with different concentrations of compounds (in triplicate) for 48 h. Cell viability is monitored using the CellTiter-Glo assay.
Animal Research:[1]
  • Animal Models: Human megakaryoblastic leukemia xenografts SET-2
  • Dosages: 150 mg/kg
  • Administration: oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 472.58
Formula

C28H32N4O3

CAS No. 937272-79-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCN(C1)CCOC2=C3COCC=CCOCC4=CC(=CC=C4)C5=NC(=NC=C5)NC(=C3)C=C2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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