Cat. No.: HY-16379

Pacritinib

Name: Pacritinib
Brand: MedChemExpress
SKU: HY-16379
Price: 115.00 USD
Availability: InStock
Rating: 5 (20 reviews)

(Synonyms: SB1518)

20 Cited Publications

고객리뷰

Based on 20 publication(s) in Google Scholar

Pacritinib (SB1518) is an orally active, selective JAK2/FLT3 inhibitor with IC₅₀ values of 23 nM and 22 nM, respectively. Pacritinib inhibits downstream STAT5, ERK1/2, and AKT signaling, and induces Apoptosis and G1 phase arrest. Pacritinib normalizes tumor-induced cytokines/chemokines, and reduces metastasis, tumor growth, shrinkage, migration, liver injury, inflammation, and steatosis. Pacritinib can be used in research on acute myeloid leukemia, myeloproliferative neoplasms, leukemia/lymphoma, GVHD, and alcoholic/non-alcoholic liver fibrosis.

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Purity : 99.88%
CAS No.: 937272-79-2
화학식: C₂₈H₃₂N₄O₃
분자량:472.58

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pacritinib Chemical Structure

CAS No.: 937272-79-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (20)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
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Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

JAK2

23 nM (IC₅₀)

FLT3

22 nM (IC₅₀)

STAT5

ERK1

ERK2

All JAK Isoforms :

All STAT Isoforms :

All ERK Isoforms :

All Akt Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.664 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human A2780 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human A2780 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
A549	IC₅₀	2.547 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
BaF3	GI₅₀	<434 nM Compound: Pacritinib	Growth inhibition of mouse BaF3 cells transfected in FLT3-TDK mutant measured after 72 hrs by CCK8 assay Growth inhibition of mouse BaF3 cells transfected in FLT3-TDK mutant measured after 72 hrs by CCK8 assay	[PMID: 35923716]
BaF3	GI₅₀	0.16 μM Compound: 21c, SB1518, 85:15 trans/cis mixture	Antiproliferative activity against mouse BA/F3 cells harboring JAK2 V617F mutation assessed as cell viability after 48 hrs by Cell titer Glo assay Antiproliferative activity against mouse BA/F3 cells harboring JAK2 V617F mutation assessed as cell viability after 48 hrs by Cell titer Glo assay	[PMID: 21604762]
BaF3	GI₅₀	0.16 μM Compound: 5; SB1518,VONJO	Growth inhibition of mouse BaF3 cells harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Growth inhibition of mouse BaF3 cells harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 38389874]
BaF3	GI₅₀	133 nM Compound: Pacritinib	Growth inhibition of mouse BaF3 cells transfected in FLT3-ITD mutant measured after 72 hrs by CCK8 assay Growth inhibition of mouse BaF3 cells transfected in FLT3-ITD mutant measured after 72 hrs by CCK8 assay	[PMID: 35923716]
BaF3	IC₅₀	0.16 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against mouse BaF3 cells harboring JAK2 V617F mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against mouse BaF3 cells harboring JAK2 V617F mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
BaF3	IC₅₀	1061.3 nM Compound: SB1518	Inhibition of JAK2 V617F mutant in BAF3 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay Inhibition of JAK2 V617F mutant in BAF3 cells assessed as reduction in cell growth measured after 72 hrs by MTT assay	[PMID: 31670517]
BaF3	IC₅₀	133 nM Compound: 21; SB1518	Cytotoxicity against mouse BaF3 cells expressing FLT3-ITD measured after 72 hrs by cell titre glo assay Cytotoxicity against mouse BaF3 cells expressing FLT3-ITD measured after 72 hrs by cell titre glo assay	[PMID: 33719439]
BaF3	IC₅₀	19 nM Compound: 21c, SB1518, 85:15 trans/cis mixture	Inhibition of JAK2 V617F mutant expressed in mouse Ba/f3 cells Inhibition of JAK2 V617F mutant expressed in mouse Ba/f3 cells	[PMID: 21604762]
BaF3	IC₅₀	291 nM Compound: 21; SB1518	Cytotoxicity against mouse BaF3 cells expressing FLT3-ITD-F691L measured after 72 hrs by cell titre glo assay Cytotoxicity against mouse BaF3 cells expressing FLT3-ITD-F691L measured after 72 hrs by cell titre glo assay	[PMID: 33719439]
BaF3	IC₅₀	306 nM Compound: 21; SB1518	Cytotoxicity against mouse BaF3 cells expressing FLT3-ITD-D835H measured after 72 hrs by cell titre glo assay Cytotoxicity against mouse BaF3 cells expressing FLT3-ITD-D835H measured after 72 hrs by cell titre glo assay	[PMID: 33719439]
BaF3	IC₅₀	434 nM Compound: 21; SB1518	Cytotoxicity against mouse BaF3 cells expressing FLT3-ITD-D835Y measured after 72 hrs by cell titre glo assay Cytotoxicity against mouse BaF3 cells expressing FLT3-ITD-D835Y measured after 72 hrs by cell titre glo assay	[PMID: 33719439]
CHL-1	IC₅₀	1.399 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human CHL-1 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human CHL-1 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
COLO 205	IC₅₀	2.615 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human COLO 205 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
HCT-116	IC₅₀	0.88 μM Compound: 2; SB1518	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 27541357]
HCT-116	IC₅₀	1.688 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
HCT-116	IC₅₀	1.69 μM Compound: 2; SB1518	Antiproliferative activity against human HCT116 cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human HCT116 cells after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
HEL	GI₅₀	1.1 μM Compound: IV; SB1518	Antiproliferative activity against human HEL cells assessed as growth inhibition after 72 hrs by CCK-8 assay Antiproliferative activity against human HEL cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 31408808]
HEL 92.1.7	IC₅₀	1.17 μM Compound: 2; SB1518	Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 36 hrs by PrestoBlue dye based assay	[PMID: 27541357]
HEL 92.1.7	IC₅₀	1.17 μM Compound: Pacritinib	Antiproliferative activity against human HEL 92.1.7 cells after 36 hrs by PrestoBlue dye based assay Antiproliferative activity against human HEL 92.1.7 cells after 36 hrs by PrestoBlue dye based assay	[PMID: 28953386]
HEL 92.1.7	IC₅₀	1.726 μM Compound: 2; SB1518	Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 48 hrs by CellTiter-Glo assay Antiproliferative activity against HEL 92.1.7 cells harboring JAK2 V617F mutant after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
HEL 92.1.7	IC₅₀	1.726 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human HEL 92.1.7 cells harboring JAK2 V617F mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human HEL 92.1.7 cells harboring JAK2 V617F mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
HL-60	GI₅₀	1.4 μM Compound: IV; SB1518	Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by CCK-8 assay Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 31408808]
HL-60	IC₅₀	0.52 μM Compound: 2; SB1518	Antiproliferative activity against human HL60 cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human HL60 cells after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
HL-60	IC₅₀	0.52 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human HL-60 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
HL-60	IC₅₀	1.78 μM Compound: 2; SB1518	Antiproliferative activity against human HL60 cells Antiproliferative activity against human HL60 cells	[PMID: 27541357]
HL-60	IC₅₀	1.78 μM Compound: Pacritinib	Antiproliferative activity against human HL60 cells Antiproliferative activity against human HL60 cells	[PMID: 28953386]
Jurkat	IC₅₀	0.839 μM Compound: 2; SB1518	Antiproliferative activity against human Jurkat cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human Jurkat cells after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
Jurkat	IC₅₀	1.09 μM Compound: 2; SB1518	Antiproliferative activity against human Jurkat cells Antiproliferative activity against human Jurkat cells	[PMID: 27541357]
Jurkat	IC₅₀	1.09 μM Compound: Pacritinib	Antiproliferative activity against human Jurkat cells Antiproliferative activity against human Jurkat cells	[PMID: 28953386]
Jurkat E6.1	IC₅₀	0.839 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human Jurkat E6.1 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human Jurkat E6.1 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
Karpas-1106P	EC₅₀	1.122 μM Compound: Chemical Probe: SB1518	Induction of apoptosis in human KARPAS-1106P cells assessed as activation of caspase-3/7 incubated for 16 hrs Induction of apoptosis in human KARPAS-1106P cells assessed as activation of caspase-3/7 incubated for 16 hrs	[PMID: 21691275]
Karpas-1106P	IC₅₀	0.348 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human KARPAS-1106P cells harboring JAK2 assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human KARPAS-1106P cells harboring JAK2 assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
KG-1	IC₅₀	1.48 μM Compound: 2; SB1518	Antiproliferative activity against human KG1 cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human KG1 cells after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
KG-1	IC₅₀	1.48 μM Compound: Pacritinib	Antiproliferative activity against human KG1 cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human KG1 cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 28953386]
KMS-12-BM	IC₅₀	0.75 μM Compound: 2; SB1518	Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
KMS-12-BM	IC₅₀	0.75 μM Compound: Pacritinib	Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human KMS-12-BM cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 28953386]
Leukemia cell	IC₅₀	0.18 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against relapsed human derived M2 Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against relapsed human derived M2 Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
Leukemia cell	IC₅₀	0.21 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against relapsed human derived M3 Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against relapsed human derived M3 Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
Leukemia cell	IC₅₀	0.24 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against human derived M5b Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against human derived M5b Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
Leukemia cell	IC₅₀	0.25 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against relapsed human derived M5b Fab type Acute myeloid leukemic cells harboring FLT3-ITD mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against relapsed human derived M5b Fab type Acute myeloid leukemic cells harboring FLT3-ITD mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
Leukemia cell	IC₅₀	0.268 μM Compound: Chemical Probe: Pacritinib, SB1518	Induction of apoptosis in human derived Acute myeloid leukemic cells assessed increase in cleaved caspase-3/7 after 16 hrs by Caspase-Glo 3/7 assay Induction of apoptosis in human derived Acute myeloid leukemic cells assessed increase in cleaved caspase-3/7 after 16 hrs by Caspase-Glo 3/7 assay	[PMID: 22829080]
Leukemia cell	IC₅₀	0.34 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against relapsed human derived M2 Fab type Acute myeloid leukemic cells harboring FLT3-ITD mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against relapsed human derived M2 Fab type Acute myeloid leukemic cells harboring FLT3-ITD mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
Leukemia cell	IC₅₀	0.35 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against human derived M2 Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against human derived M2 Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
Leukemia cell	IC₅₀	0.46 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against human derived Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against human derived Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
Leukemia cell	IC₅₀	0.46 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against relapsed human derived M5b Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against relapsed human derived M5b Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
Leukemia cell	IC₅₀	0.84 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against human derived M4 Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against human derived M4 Fab type Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
Leukemia cell	IC₅₀	1.33 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against relapsed human derived Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against relapsed human derived Acute myeloid leukemic cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
LN-18	CC₅₀	>1 μM Compound: 44	Cytotoxicity against human LN-18 cells Cytotoxicity against human LN-18 cells	[PMID: 33539089]
LNCaP	IC₅₀	0.917 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human LNCaP cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human LNCaP cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
MCF7	IC₅₀	0.29 μM Compound: 2; SB1518	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 27541357]
MCF7	IC₅₀	0.85 μM Compound: 2; SB1518	Antiproliferative activity against human MCF7 cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MCF7 cells after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
MCF7	IC₅₀	0.853 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
MDA-MB-231	IC₅₀	2.43 μM Compound: 2; SB1518	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27541357]
MKN-7	IC₅₀	2.042 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human MKN-7 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human MKN-7 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
MOLM-13	GI₅₀	173 nM Compound: Pacritinib	Growth inhibition of human MOLM-13 cells harboring FLT3 resistant inhibitor assessed as growth inhibition Growth inhibition of human MOLM-13 cells harboring FLT3 resistant inhibitor assessed as growth inhibition	[PMID: 35923716]
MOLM-13	GI₅₀	73 nM Compound: Pacritinib	Growth inhibition of human MOLM-13 cells by WST-8 assay Growth inhibition of human MOLM-13 cells by WST-8 assay	[PMID: 35923716]
MOLM-13	IC₅₀	0.067 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
MOLM-13	IC₅₀	173 nM Compound: 21; SB1518	Cytotoxicity against human MOLM-13 cells expressing FLT3-D835Y measured after 72 hrs by cell titre glo assay Cytotoxicity against human MOLM-13 cells expressing FLT3-D835Y measured after 72 hrs by cell titre glo assay	[PMID: 33719439]
MOLM-13	IC₅₀	47 nM Compound: 3; SB1518	Antiproliferative activity against human MOLM13 cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM13 cells after 48 hrs by CellTiter-Glo assay	[PMID: 31207462]
MOLM-13	IC₅₀	67 nM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against human MOLM-13 cells harboring FLT3-ITD mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
MOLM-13	IC₅₀	73 nM Compound: 21; SB1518	Cytotoxicity against human MOLM-13 cells measured after 72 hrs by cell titre glo assay Cytotoxicity against human MOLM-13 cells measured after 72 hrs by cell titre glo assay	[PMID: 33719439]
MOLM-14	IC₅₀	0.079 μM Compound: 2; SB1518	Antiproliferative activity against human MOLM14 cells harboring FLT3-ITD mutant after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MOLM14 cells harboring FLT3-ITD mutant after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
MOLM-14	IC₅₀	0.079 μM Compound: Pacritinib	Antiproliferative activity against human MOLM14 cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human MOLM14 cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 28953386]
MOLT-4	IC₅₀	0.75 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
MV4-11	EC₅₀	0.96 μM Compound: Chemical Probe: Pacritinib, SB1518	Induction of apoptosis in human MV4-11 cells harboring FLT3-ITD mutant assessed increase in cleaved caspase-3/7 after 16 hrs by Caspase-Glo 3/7 assay Induction of apoptosis in human MV4-11 cells harboring FLT3-ITD mutant assessed increase in cleaved caspase-3/7 after 16 hrs by Caspase-Glo 3/7 assay	[PMID: 22829080]
MV4-11	GI₅₀	0.047 μM Compound: 21c, SB1518, 85:15 trans/cis mixture	Antiproliferative activity against human MV4-11 cells harboring FLT3 D835Y mutant assessed as cell viability after 48 hrs by Cell titer Glo assay Antiproliferative activity against human MV4-11 cells harboring FLT3 D835Y mutant assessed as cell viability after 48 hrs by Cell titer Glo assay	[PMID: 21604762]
MV4-11	GI₅₀	0.047 μM Compound: 5; SB1518,VONJO	Growth inhibition of human MV4-11 cells by WST-8 assay Growth inhibition of human MV4-11 cells by WST-8 assay	[PMID: 38389874]
MV4-11	GI₅₀	1.6 μM Compound: IV; SB1518	Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 31408808]
MV4-11	GI₅₀	33 nM Compound: Pacritinib	Growth inhibition of human MV4-11 cells by WST-8 assay Growth inhibition of human MV4-11 cells by WST-8 assay	[PMID: 35923716]
MV4-11	IC₅₀	0.047 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
MV4-11	IC₅₀	47 nM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells harboring FLT3-ITD mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
MV4-11	IC₅₀	6 nM Compound: 21c, SB1518, 85:15 trans/cis mixture	Inhibition of FLT3 D835Y mutant expressed in human MV4-11 cells Inhibition of FLT3 D835Y mutant expressed in human MV4-11 cells	[PMID: 21604762]
MV4-11	IC₅₀	67 nM Compound: 3; SB1518	Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human MV4-11 cells after 48 hrs by CellTiter-Glo assay	[PMID: 31207462]
NCI-H322M	IC₅₀	2.18 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human NCI-H322M cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human NCI-H322M cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
OPM-2	IC₅₀	1.21 μM Compound: 2; SB1518	Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
OPM-2	IC₅₀	1.21 μM Compound: Pacritinib	Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human OPM2 cells after 48 hrs by CellTiter-Glo luminescent assay	[PMID: 28953386]
PC-3	IC₅₀	0.77 μM Compound: 2; SB1518	Antiproliferative activity against human PC3 cells after 48 hrs by CellTiter-Glo assay Antiproliferative activity against human PC3 cells after 48 hrs by CellTiter-Glo assay	[PMID: 27541357]
PC-3	IC₅₀	0.77 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
PC-3	IC₅₀	2.41 μM Compound: 2; SB1518	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 27541357]
RS4-11	IC₅₀	930 nM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against human RS4-11 cells assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
SET-2	EC₅₀	0.571 μM Compound: Chemical Probe: SB1518	Induction of apoptosis in human SET2 cells assessed as activation of caspase-3/7 incubated for 16 hrs Induction of apoptosis in human SET2 cells assessed as activation of caspase-3/7 incubated for 16 hrs	[PMID: 21691275]
SET-2	IC₅₀	0.217 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human SET2 cells harboring JAK2 V617F mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human SET2 cells harboring JAK2 V617F mutant assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
SET-2	IC₅₀	0.22 μM Compound: Chemical Probe: Pacritinib, SB1518	Antiproliferative activity against human SET2 cells harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay Antiproliferative activity against human SET2 cells harboring JAK2 V617F mutant assessed as reduction in cell viability incubated for 48 hr by CellTiter-Glo assay	[PMID: 22829080]
SET-2	IC₅₀	915.7 nM Compound: SB1518	Antiproliferative activity against human SET2 cells overexpressing JAK2 V716F mutant assessed as reduction in cell growth after 72 hrs by MTT assay Antiproliferative activity against human SET2 cells overexpressing JAK2 V716F mutant assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 31670517]
SNU-387	IC₅₀	2.03 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human SNU-387 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human SNU-387 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
SNU-475	IC₅₀	2.44 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human SNU-475 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human SNU-475 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
T47D	IC₅₀	1.275 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human T47D cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human T47D cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]
TAMH	IC₅₀	3.68 μM Compound: 2; SB1518	Antiproliferative activity against mouse TAMH cells after 24 hrs by CellTiter-Glo assay Antiproliferative activity against mouse TAMH cells after 24 hrs by CellTiter-Glo assay	[PMID: 27541357]
TAMH	IC₅₀	3.68 μM Compound: Pacritinib	Cytotoxicity against TAMH cells assessed as cell viability after 24 hrs by CellTiter-Glo assay Cytotoxicity against TAMH cells assessed as cell viability after 24 hrs by CellTiter-Glo assay	[PMID: 28953386]
U-266	IC₅₀	1.35 μM Compound: Chemical Probe: SB1518	Antiproliferative activity against human U-266 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay Antiproliferative activity against human U-266 cells assessed as inhibition of cell viability incubated for 48 hrs by CellTiterGlo assay	[PMID: 21691275]

In Vitro

Anti-cancerApoptosisInnate ImmunityAdaptive ImmunityCytokines & ChemokinesImmune Tolerance & ImmunosuppressionOthers

Anti-cancer

Pacritinib (up to 10 μM; 48 h) inhibits proliferation of AML cell lines, with IC₅₀ values of 47 nM in MV4-11, 67 nM in MOLM-13, 220 nM in SET-2, and 930 nM in RS4;11^[1].
Pacritinib (8-1000 nM; 3 h) inhibits FLT3 autophosphorylation and downstream STAT5, MAPK, and PI3K signaling in FLT3-ITD and FLT3-wt AML cell lines, with pSTAT5 IC₅₀ values of 40 nM in MV4-11, 20 nM in MOLM-13, and 8 nM in RS4;11^[1].
Pacritinib inhibits the proliferation of leukemia and lymphoma cell lines dependent on JAK2 or FLT3 activation, with an IC₅₀ of 35-240 nM^[4].
Pacritinib inhibits JAK/STAT signaling and proliferation in cancer cell lines, including Karpas 1106P and Karpas1160, with an IC₅₀ of 110 ng/mL for Karpas1160 proliferation^[7].

Apoptosis

Pacritinib (0.5 nM-10 μM; 16 h) induces caspase-3/7 activation in MV4-11 cells with an EC₅₀ of 0.96 μM^[1].
Pacritinib (0.03-0.15 μM; 48-72 h) dose-dependently increases early and late apoptosis in MV4-11 cells without inducing necrosis^[1].
Pacritinib combined with Pracinostat (HY-13322) completely eliminates JAK2 autophosphorylation in SET-2 cells and enhances apoptosis markers in SET-2, HEL92.1.7, MV4-11, and MOLM-13 cells^[2].

Innate Immunity

Adaptive Immunity

Cytokines & Chemokines

Pacritinib combined with Sirolimus (HY-10219) inhibits the production of IFNγ, IL13, and GMCSF in DC alloantigen-stimulated human T cells^[5].

Adaptive Immunity

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

Anti-cancer

Pacritinib (10 µM; 5-7 days) inhibits TH1, TH17, and Treg differentiation and CFSE-based T cell proliferation in MNC cultures from MPN samples and normal controls^[6].

Others

Pacritinib has comparable potency against JAK2 and FLT3 in cell-free kinase assays, with IC₅₀ values of 23 nM and 22 nM, respectively^[1].
Pacritinib (1 μM; 24 h) reduces fibrosis marker expression and proliferation in primary mouse wild-type and SM22Cre⁺-Jak2f/f HSCs as well as LX-2 and TWNT-4 HSCs, with JAK2-dependent effects in mouse HSCs^[3].
Pacritinib inhibits JAK2, JAK2 V617F, FLT3, and FLT3 D835Y with IC₅₀ values of 6-22 nM^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

AML cell lines, including SET-2, MV4-11, MOLM-13, RS4;11, and other AML-derived lines
Concentration:

up to 10 μM
Incubation Time:

48 h
Result:

Showed the highest potency in FAB M5 subtype lines (THP-1, MV4-11, and MOLM-13).
SET-2 (JAK2V617F) IC₅₀ = 0.22 μM; MV4-11 IC₅₀ = 47 nM; MOLM-13 IC₅₀ = 67 nM; RS4;11 IC₅₀ = 930 nM; MV4-11-P IC₅₀ = 153 nM; MV4-11-R IC₅₀ = 434 nM, a 2.9-fold difference between parental and resistant cells.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.5 nM-10 μM
Incubation Time:

16 h
Result:

Dose-dependently activated caspase-3/7, with an EC₅₀ of 0.96 μM.

Apoptosis Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.03 and 0.15 μM
Incubation Time:

48 h and 72 h
Result:

At 48 h, 0.03 mM increased early and late apoptotic cells to 24.50% and 5.58%, respectively; 0.15 mM increased them to 39.39% and 20.83%.
At 72 h, 0.03 mM increased early and late apoptotic cells to 22.69% and 3.74%; 0.15 mM increased them to 58.69% and 15.10%.
No necrosis induction was observed.

Western Blot Analysis^[1]

Cell Line:

MV4-11, MOLM-13, and RS4;11 cells
Concentration:

8, 40, 200, 1000 nM
Incubation Time:

3 h (MOLM-13 and RS4;11 plus 10 ng/mL FLT3 ligand for 3 min)
Result:

In MV4-11, dose-dependent decreases occurred in pFLT3, pSTAT5, pERK1/2, and pAkt with IC₅₀ values of 80, 40, 33, and 29 nM, respectively.
In MOLM-13, IC₅₀ values were 180 nM for pFLT3 and 20 nM for pSTAT5.
In RS4;11, IC₅₀ values were 600 nM for pFLT3 and 8 nM for pSTAT5.

In Vivo

Anti-cancerCytokines & ChemokinesAdaptive ImmunityImmune Tolerance & ImmunosuppressionOthers

Anti-cancer

Pacritinib (Pacritinib hydrochloride; 25-100 mg/kg; once daily; for 21 consecutive days) produces dose-dependent tumor growth inhibition and complete regression in the MV4-11 AML xenograft model^[1].
Pacritinib (Pacritinib hydrochloride; 150 mg/kg; oral; twice daily; for 7 consecutive days) inhibits MOLM-13 tumor growth and reduces lung metastasis in the MOLM-13 AML xenograft model in vivo^[1].
Pacritinib (oral) demonstrates target inhibition and antitumor activity in the MV4-11 leukemia model in nude mice^[4].

Anti-cancer

Cytokines & Chemokines

Pacritinib (150 mg/kg; oral; twice daily; 19 days (d0-d18)) inhibits SET-2 AML xenograft tumor growth, reduces pSTAT5 and the incidence of lymph node metastasis, and normalizes plasma levels of IL-6, IP-10, and KC^[2].

Adaptive Immunity

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

Pacritinib (50 mg/kg; 14 days) reduces pathogenic CD4⁺ pSTAT3⁺ and Th1/Th17 cells and preserves Tregs in xenogeneic GVHD NSG mice, and PAC/SIR (50 mg/kg plus sirolimus; 14 days) improves survival and GVHD scores^[5].

Others

Pacritinib (65 μg/kg; intravenous injection; twice weekly; 4 weeks) attenuates liver injury and fibrosis in the CCl₄/ethanol-induced ASH mouse model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c nude (BALB/cOlaHsd-Foxn1nu; female; athymic; 9-16 weeks of age at tumor implantation)^[1]
Dosage:

25 mg/kg, 50 mg/kg, and 100 mg/kg (efficacy); 150 mg/kg (target engagement)
Administration:

oral; once daily; 21 consecutive days; single dose (target engagement)
Result:

Induced dose-dependent tumor growth inhibition: 38% at 25 mg/kg, 92% at 50 mg/kg, and 121% at 100 mg/kg.
Complete regression was observed in 3/10 mice at 50 mg/kg/day and 8/8 mice at 100 mg/kg/day.
A single 150 mg/kg dose blocked FLT3 and downstream signaling in tumor tissues at 2 and 4 h; pSTAT5 (Y694) was decreased in tumor lysates at 2 and 4 h compared with vehicle.

Animal Model:

C.B-17/IcrHan (Hsd-Prkdcscid; female; severe combined immunodeficiency)^[1]
Dosage:

150 mg/kg (efficacy); 150 mg/kg (target engagement)
Administration:

oral; b.i.d.; 7 consecutive days (methods state 8 consecutive days); single dose (target engagement)
Result:

Dosing resulted in 83% tumor growth inhibition after 7 days of dosing.
Metastatic incidence (mostly in the lungs) was reduced from 0.83 to 0.33 in the high-dose pacritinib group.
A single 150 mg/kg dose blocked FLT3 and downstream signaling at 3 h; in tumor lysates, pSTAT5 (Y694) was fully inhibited 3 h after the last dose on day 7.

Animal Model:

C.B-17.Cg-PrkdcscidLystbg/Crl (female, 9 weeks old)^[2]
Dosage:

150 mg/kg (doses refer to free base)
Administration:

p.o. gavage; twice daily; for 19 days (d0-d18)
Result:

Led to 61% tumor growth inhibition based on tumor volume and 47% tumor growth inhibition based on tumor weight.
pSTAT5 levels in tumors were decreased by about 50% after chronic monotherapy.
No lymph node metastases were observed in mice dosed with pacritinib alone.
Plasma MCP-1 levels in tumor-bearing mice were reduced by 10% after pacritinib monotherapy; IL-6, IP-10, and KC were normalized.

Animal Model:

C57BL/6J (wild-type, male, 10-12 weeks old)^[3]
Dosage:

65 μg/kg body weight
Administration:

i.v. injection; twice per week; starting 3 weeks after first CCl4 injection for 4 weeks
Result:

Reduced serum ALT levels.
Reduced serum AST levels.
Improved liver parenchyma by H&E staining.
Decreased Sirius red collagen staining.
α-SMA immunostaining showed a trend toward reduction.
Collagen-1 and p-moesin protein levels were reduced.
Col1a1 mRNA expression showed a trend toward reduction, while Acta2 and Tgfb showed no changes.
No changes were observed in steatosis markers, oil red O staining, hepatic triglyceride content, or liver-to-body weight ratio.

Animal Model:

NSG (male or female, age 6 to 24 weeks old)^[5]
Dosage:

50 mg/kg (PAC); 50 mg/kg plus sirolimus (PAC/SIR)
Administration:

for 14 days
Result:

Decreased the frequency of CD4+, pSTAT3+ human T cells in mouse spleens at day 14.
Increased the amount of Tregs in mouse spleen at day 14.
Improved survival from xenogeneic GVHD compared with either inhibitor alone.
Reduced GVHD scores.
Decreased the frequency of CD4+, pSTAT3+ human T cells at day 14.
Decreased CD4+, pS6+ T cells at day 14.
Decreased both CD4+, pSTAT3+ and pS6+ T cells.
Decreased the frequency of pathogenic Th1 cells in the spleen at day 14.
Decreased human Th17 cells at day 14.
Had similar Th2 cell frequency.
Did not increase Treg frequency in mice transplanted with standard human PBMCs.
In mice transplanted with Treg-depleted PBMCs, PAC/SIR produced more human Tregs at day 14 in mouse spleens compared with sirolimus.
PAC/SIR-treated mice retained high frequencies of CD4+, pH3ser10+ T cells compared with controls.

Related Protocols :

Chemical Information

CAS No. 937272-79-2
Appearance Solid
분자량 472.58
화학식 C₂₈H₃₂N₄O₃
Color Light yellow to yellow
SMILES

C1(COC/C=C/COCC2=C(OCCN3CCCC3)C=CC4=C2)=CC=CC(C5=N/C(NC=C5)=N\4)=C1
Synonyms

SB1518
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (20)

All WBRT-PCRIn Vivo Efficacy StudyCell Proliferation/Viability Assay

Sort by:

Journal Impact Factor

Nat Med

Chromosome 1q21.3 amplification is a trackable biomarker and actionable target for breast cancer recurrence. [Abstract]

2017 Nov;23(11):1319-1330. PMID: 28967919

Pacritinib purchased from MedChemExpress. Usage Cited in: Nat Med. 2017 Nov;23(11):1319-1330. [Abstract]

Pacritinib effectively disrupts the S100A7/8/9–IRAK1 feedback loop to inhibit tumorsphere growth. Representative western blot (n=2) showing inhibition of phosphorylated IRAK1 and phosphorylated JAK2 (pJAK2) within 6 h of Pacritinib treatment in MB468 and MB231 cells. Actin is used as a loading control.
Science

Antifibrotic drug finerenone restores fertility in premature ovarian insufficiency. [Abstract]

2026 Feb 5;391(6785):eadz4075. PMID: 41643022
Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Nat Commun

Genotoxic stress and viral infection induce transient expression of APOBEC3A and pro-inflammatory genes through two distinct pathways. [Abstract]

2021 Aug 13;12(1):4917. PMID: 34389714

Pacritinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]

Pacritinib (0.25-1 µM; 6 h) treatment caused inhibition of phosphorylated IRAK1 and phosphorylated JAK2 (pJAK2) in MB468 and MB231 cells.

Pacritinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]

Real-time PCR analysis of S100A7, S100A8, and S100A9 gene expression after Pacritinib (0.25-1 µM; 24 h) treatment in MB468 cells.

Pacritinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]

NOD-SCID mice bearing MB231 and HCC70 tumors were treated with pacritinib (50, 100, or 150 mg/kg; p.o.; once daily for 21 d). Pacritinib treatment in different doses resulted in substantial inhibition of tumor growth for HCC70 xenograft tumors but had no obvious effect on the growth of MB231 xenografts.

Pacritinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]

Growth curve of tumorspheres from ER-positive and ER-negative breast cancer cell lines treated with increasing doses of Pacritinib (0.25-5 µM). Pacritinib treatment was more effective in impairment of tumorsphere growth in cancer cell lines positive for 1q21.3 amplification than in cell lines without amplification.
Nat Commun

Stromal induction of BRD4 phosphorylation Results in Chromatin Remodeling and BET inhibitor Resistance in Colorectal Cancer. [Abstract]

2021 Jul 21;12(1):4441. PMID: 34290255
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Death Dis

Colorectal cancer-associated fibroblasts promote metastasis by up-regulating LRG1 through stromal IL-6/STAT3 signaling. [Abstract]

2021 Dec 20;13(1):16. PMID: 34930899
Mol Cancer Ther

2026 Jul 14. PMID: 42442343
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Inflamm Res

Potent repression of C-reactive protein (CRP) expression by the JAK1/2 inhibitor ruxolitinib in inflammatory human hepatocytes. [Abstract]

2020 Jan;69(1):51-62. PMID: 31654094
Drug Des Devel Ther

Advances in the drug therapies of acute myeloid leukemia (except acute wpromyelocytic leukemia). [Abstract]

2018 Apr 30:12:1009-1017. PMID: 29750014
Eur J Pharmacol

VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]

2025 Sep 15:1003:177942. PMID: 40651787
PLoS Pathog

Kaposi sarcoma-associated herpesvirus cooperates with Epstein-Barr virus to co-transform a small set of human B cells oncogenically. [Abstract]

2025 Jun 23;21(6):e1013281. PMID: 40549805
PLoS Genet

Her2 amplification, Rel-A, and Bach1 can influence APOBEC3A expression in breast cancer cells. [Abstract]

2024 May 28;20(5):e1011293. PMID: 38805570
BMJ Open Ophthalmol

Impact of anticancer drugs on human Tenon's fibroblast proliferation: implications for glaucoma surgery. [Abstract]

2026 Jan 12;11(1):e002307. PMID: 41526033
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
bioRxiv

2025 June 03.
bioRxiv

2025 February 21.
Patent

US20220323444A1.

용액&용해도

In Vitro:

1 M HCl : ≥ 100 mg/mL (211.60 mM)

DMSO : 10 mg/mL (21.16 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

0.1 M HCl : 2 mg/mL (4.23 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1160 mL

10.5802 mL

21.1604 mL

5 mM

0.4232 mL

2.1160 mL

4.2321 mL

10 mM

0.2116 mL

1.0580 mL

2.1160 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기

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Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1 mg/mL (2.12 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 1 mg/mL (2.12 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 0.3 mg/mL (0.63 mM); Clear solution

In Vivo Dissolution Calculator

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

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References

[1]. Hart S, et al. Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia. Blood cancer journal. 2011 Nov;1(11):e44. [Content Brief]

[2]. Novotny-Diermayr V, et al. The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML. Blood cancer journal. 2012 May;2(5):e69. [Content Brief]

[3]. Torres S, et al. Janus kinase 2 inhibition by pacritinib as potential therapeutic target for liver fibrosis. Hepatology (Baltimore, Md.). 2023 Apr 01;77(4):1228-1240.

[4]. Hart S, et al. Pharmacodynamic (PD) Biomarker Assay Validation for SB1518, a Novel Oral JAK2 Inhibitor in Phase 1 Clinical Trials for Advanced Leukemias, Myeloproliferative Diseases and Lymphoma. Blood. 2009 Nov 20;114(22):1888.

[5]. Pidala J, et al. Pacritinib Combined with Sirolimus and Low-Dose Tacrolimus for GVHD Prevention after Allogeneic Hematopoietic Cell Transplantation: Preclinical and Phase I Trial Results. Clinical cancer research : an official journal of the American Association for Cancer Research. 2021 May 15;27(10):2712-2722.

[6]. Chen C, et al. Comparison of Ruxolitinib, Momelotinib, and Pacritinib in the Inhibition of Immune Differentiation and Proliferation of T Cells in Myeloproliferative Neoplasm. Blood. 2015 Dec 3;126(23):5203.

[7]. Younes A, et al. Phase I study of a novel oral Janus kinase 2 inhibitor, SB1518, in patients with relapsed lymphoma: evidence of clinical and biologic activity in multiple lymphoma subtypes. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2012 Nov 20;30(33):4161-7.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
0.1 M HCl / DMSO / 1 M HCl	1 mM	2.1160 mL	10.5802 mL	21.1604 mL	52.9011 mL
DMSO / 1 M HCl	5 mM	0.4232 mL	2.1160 mL	4.2321 mL	10.5802 mL
	10 mM	0.2116 mL	1.0580 mL	2.1160 mL	5.2901 mL
	15 mM	0.1411 mL	0.7053 mL	1.4107 mL	3.5267 mL
	20 mM	0.1058 mL	0.5290 mL	1.0580 mL	2.6451 mL
1 M HCl	25 mM	0.0846 mL	0.4232 mL	0.8464 mL	2.1160 mL
	30 mM	0.0705 mL	0.3527 mL	0.7053 mL	1.7634 mL
	40 mM	0.0529 mL	0.2645 mL	0.5290 mL	1.3225 mL
	50 mM	0.0423 mL	0.2116 mL	0.4232 mL	1.0580 mL
	60 mM	0.0353 mL	0.1763 mL	0.3527 mL	0.8817 mL
	80 mM	0.0265 mL	0.1323 mL	0.2645 mL	0.6613 mL
	100 mM	0.0212 mL	0.1058 mL	0.2116 mL	0.5290 mL

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Pacritinib

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Pacritinib

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