Pacritinib
Based on 19 publication(s) in Google Scholar
Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM).
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 937272-79-2
- Formula: C28H32N4O3
- Molecular Weight:472.58
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Pacritinib
More- Nat Med. 2017 Nov;23(11):1319-1330. [Abstract]
- Science. 2026 Feb 5;391(6785):eadz4075. [Abstract]
- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Nat Commun. 2021 Aug 13;12(1):4917. [Abstract]
- Nat Commun. 2021 Jul 21;12(1):4441. [Abstract]
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Cell Death Dis. 2021 Dec 20;13(1):16. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Inflamm Res. 2020 Jan;69(1):51-62. [Abstract]
- Drug Des Devel Ther. 2018 Apr 30:12:1009-1017. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177942. [Abstract]
- PLoS Pathog. 2025 Jun 23;21(6):e1013281. [Abstract]
- PLoS Genet. 2024 May 28;20(5):e1011293. [Abstract]
- BMJ Open Ophthalmol. 2026 Jan 12;11(1):e002307. [Abstract]
- Fundam Clin Pharmacol. 2021 Oct;35(5):919-929. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2021 Sep;46(5):625-635. [Abstract]
- bioRxiv. 2025 June 03.
- bioRxiv. 2025 February 21.
- Patent. US20220323444A1.
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WB
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RT-PCR
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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WB
Biological Activity
|
JAK2V617F 19 nM (IC50) |
JAK2wt 23 nM (IC50) |
Tyk2 50 nM (IC50) |
JAK3 520 nM (IC50) |
JAK1 1280 nM (IC50) |
FLT3D835Y 6 nM (IC50) |
FLT3wt 22 nM (IC50) |
|
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
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[PMID: 31408808] |
| MV4-11 | GI50 |
33 nM
Compound: Pacritinib
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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
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[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
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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] |
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 (Km). 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-JAK2V617F 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 937272-79-2
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Appearance Solid
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Molecular Weight 472.58
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Formula C28H32N4O3
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Color Light yellow to yellow
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SMILES
C1(COC/C=C/COCC2=C(OCCN3CCCC3)C=CC4=C2)=CC=CC(C5=N/C(NC=C5)=N\4)=C1
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Synonyms
SB1518
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (19)
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Journal Impact Factor
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Most Recent
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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.
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Science
2026 Feb 5;391(6785):eadz4075. PMID: 41643022 -
Science
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.
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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
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 -
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Solvent & Solubility
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
SET-2 and Karpas 1106P cells, and Ba/F3-JAK2V617F-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.
Mice[1]
Female athymic BALB/c nude mice (BALB/cOlaHsd-Foxn1nu) of age 12 weeks are used; and female SCID Beige mice (CB17.Cg-PrkdcscidLystbg/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.
Purity & Documentation
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Data Sheet (288 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |