Art. -Nr.: HY-16379

Pacritinib

(Synonyms: SB1518)

19 Cited Publications

Kundenbewertung

Based on 19 publication(s) in Google Scholar

Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC₅₀=23 nM) and JAK2^V617F mutant (IC₅₀=19 nM). Pacritinib also inhibits FLT3 (IC₅₀=22 nM) and its mutant FLT3^D835Y (IC₅₀=6 nM).

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Reinheit: 99.88%
CAS. Nr.: 937272-79-2
Formel: C₂₈H₃₂N₄O₃
Molecular Weight:472.58

Speicherung:

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

Pacritinib Chemical Structure

CAS. Nr.: 937272-79-2

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (19)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
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Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

JAK2^V617F

19 nM (IC₅₀)

JAK2^wt

23 nM (IC₅₀)

Tyk2

50 nM (IC₅₀)

JAK3

520 nM (IC₅₀)

JAK1

1280 nM (IC₅₀)

FLT3^D835Y

6 nM (IC₅₀)

FLT3^wt

22 nM (IC₅₀)

Alle JAK Isoform-spezifische Produkte anzeigen :

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

Relative to JAK2, Pacritinib (SB1518) 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). The rest of the evaluated kinases show <30% inhibition when tested against 100 nM Pacritinib at adenosine triphosphate concentrations equivalent to its Michaelis constant (K_m). Pacritinib inhibits MV4-11 and MOLM-13 cells (both of which are cell lines derived from human acute myeloid leukemias driven by an FLT3 ITD mutation) with IC₅₀ of 47 and 67 nM, respectively. Pacritinib inhibits Karpas 1106P and Ba/F3-JAK2^V617F cells (which are cell lines dependent on JAK2 signaling) with IC₅₀ of 348 and 160 nM, respectively^[1]. FLT3-ITD harboring MV4-11 cells are treated for 3 h with different concentrations of Pacritinib (SB1518) and pFLT3, pSTAT5 and pERK1/2 levels are quantified. Pacritinib leads to a dose-dependent decrease of pFLT3, pSTAT5, pERK1/2 and pAkt with IC₅₀ of 80, 40, 33 and 29 nM, respectively. The IC₅₀ on auto-phosphorylation of FLT3-wt in RS4;11 is four-fold higher (IC₅₀=600 nM) compare with FLT3-ITD in MV4-11 and MOLM-13 cells. However, STAT5 inhibition is detected at much lower concentrations of Pacritinib (IC₅₀=8 nM)^[2].

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

In Vivo

For evaluation of efficacy in the Ba/F3-JAK2^V617F engraftment model, mice are treated with Pacritinib (SB1518) at doses of 50 or 150 mg/kg p.o. q.d. for 13 days, with drug dosing starting 4 days after cell inoculation. At study termination, the vehicle control mice exhibit splenomegaly and hepatomegaly (~7- and 1.3-fold, respectively), reminiscent of the symptoms found in patients with symptomatic myelofibrosis. SB1518 treatment at 150 mg/kg p.o. q.d. significantly ameliorates all these symptoms, with 60% (±9%) normalization of spleen weight and 92% (±5%) normalization of liver weight and is well tolerated without significant weight loss or any hematological toxicities, including thrombocytopenia and anemia^[1]. In rats, Pacritinib (SB1518) shows moderately fast absorption (t_max=4 h), with a peak concentration of 114 ng/mL, AUC of 599 ng?h/mL, and a terminal half-life of ~6 h following a single oral dose of 10 mg/kg. In dogs, Pacritinib (SB1518) is rapidly absorbed (t_max=2.0 h), with a peak concentration of ~12 ng/mL, AUC of 53 ng?h/mL, and a terminal half-life of 3.4 h following a single oral dose of 3 mg/kg^[3].

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

Chemical Information

CAS. Nr. 937272-79-2
Appearance Solid
Molecular Weight 472.58
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (19)

All WBRT-PCRIn Vivo Efficacy StudyCell Proliferation/Viability Assay

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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 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.

Lösungsmittel & Löslichkeit

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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

Protokoll

Kinase Assay^[1]

All assays are carried out in 384-well white microtiter plates. Compounds (e.g., Pacritinib) are 4-fold serially diluted in 8 steps, starting from 10 µM. The reaction mixture consist 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 contain 2.0 µg/mL FLT3 enzyme, 5 µM of poly(Glu,Tyr) substrate and 4 µM of ATP. For JAK1 assays, the reaction contain 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 contain 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 contain 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 contain 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^[1].

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

Cell Assay^[1]

SET-2 and Karpas 1106P cells, and Ba/F3-JAK2^V617F-GFP-Luc cells are used. For proliferation assays in 96-well plates, cells are seeded at 30-50% confluency and are treated the following day with compounds (e.g., Pacritinib) (in triplicate) at concentrations up to 10 μM for 48 h. Cell viability is monitored using the CellTiter-Glo assay. Dose-response curves are plotted to determine IC₅₀ values for the compounds using the XL-fit software^[1].

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

Animal Administration^[1]^[3]

Mice^[1]
Female athymic BALB/c nude mice (BALB/cOlaHsd-Foxn1^nu) of age 12 weeks are used; and female SCID Beige mice (CB17.Cg-Prkdc^scidLyst^bg/Crl) of age 9-10 weeks are used. For the SET-2 leukemia model, 5×10⁶ tumor cells are injected subcutaneously in the right flank of severe combined immunodeficient beige mice. The cells are resuspended in 50 μL serum-free growth medium, mixed 1:1 with Matrigel and injected in a total volume of 100 μL. Tumor volumes are determined by caliper measurements and drug treatment is initiated after 31 days when tumors have reached a mean volume of 280 mm³ (tumor volume (mm³)=(w²×l)/2). This study is performed using 12 mice per group and animals are killed 3 h post-dose on day 18. Tumor growth inhibition is calculated. For the efficacy studies, mice are treated by oral gavage (10 mL/kg body weight) with doses from 50 to 150 mg/kg SB1518.
Rats and Dogs^[3]
Male Wistar rats (aged 6-8 weeks, weighing 270 to 325 g) and male Beagle dogs (6 to 7 months of age, weighing 9-11 kg) are used in this study. The oral doses for dogs and rats are 3, and 10 mg/kg, respectively. The doses are administered, by gavage, as suspensions (0.5 % methylcellulose and 0.1%tween 80) to rats, and as gelatin capsules to dogs. Following oral dosing, serial blood samples are collected (jugular vein in dogs, and superior vena cava in rats) at different time points (0 to 24 h) in tubes containing K₃EDTA as anticoagulant, and centrifuged, the plasma is separated and stored at -70°C until analysis. Plasma samples are processed and analyzed by LC/MS/MS. Pharmacokinetic parameters are estimated by noncompartmental methods using WinNonlin.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hart S, et al. SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies. Leukemia. 2011 Nov;25(11):1751-9. [Content Brief]

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

[3]. William AD, et al. Discovery of the macrocycle 11-(2-pyrrolidin-1-yl-ethoxy)-14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8,10,12(27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JA [Content Brief]

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

Keywords

Pacritinib

19 Cited Publications

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Pacritinib

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Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Pacritinib Related Classifications

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