Pacritinib

SKU: orb1301145

Description

Pacritinib

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	937272-79-2
MW	472.58
Purity	99.49%
Formula	C₂₈H₃₂N₄O₃
SMILES	C(CN1CCCC1)Oc1ccc2Nc3nccc(n3)-c3cccc(COC\C=C\COCc1c2)c3
Target	FLT,JAK,Tyrosine Kinases
Solubility	H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.12 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:3.57 mg/mL (7.55 mM)

Bioactivity

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Target IC50	Tyk2:50 nM\|JAK3:520 nM\|JAK1:1280 nM\|FLT3 (WT):22 nM\|JAK2-WT:23 nM\|FLT3 (D835Y):6 nM\|JAK2 (V617F):19 nM
In Vivo	In JAK2V617F-dependent xenograft model, Pacritinib (150 mg/kg, p.o., q.d.) markedly ameliorates splenomegaly and hepatomegaly symptoms, with 60% normalization of spleen weight and 92% normalization of liver weight and is well tolerated without significant weight loss or any hematological toxicities, including thrombocytopenia and anemia. In JAK2V617F-dependent SET-2 xenograft model, Pacritinib dose-dependent inhibits tumor growth (40% for 75 mg/kg and 61% for 150 mg/kg). Pacritinib treated once daily for 21 consecutive days, induces dose-dependent inhibition of tumor growth (38% for 25 mg/kg, 92% for 50 mg/kg and 121% for 100 mg/kg). Complete regression is observed in 3/10 and 8/8 mice for the 50 and 100 mg/kg/day groups, respectively. Read more...
In Vitro	Pacritinib is an effective inhibitor of both wild-type JAK2 and JAK2V617F mutant (IC50: 19 nM). The IC50s of Pacritinib are 50 nM for TYK2, 520 nM for JAK3 and 1280 nM for JAK1. Pacritinib effectively permeates cells to modulate signaling pathways downstream of JAK2, whether agonist activated or mutationally activated. Pacritinib induces apoptosis, cell cycle arrest and antiproliferative effects in JAK2WT- and JAK2V617F-dependent cells. Pacritinib inhibits cell proliferation of Karpas 1106P (IC50: 348 nM ) and Ba/F3-JAK2V617F (IC50: 160 nM ), respectively. Pacritinib inhibits endogenous colony growth derived from erythroid (IC50: 63 nM) and myeloid progenitors(IC50: 53 nM), respectively. SB1518 also inhibits FLT3 and its mutant FLT3-D835Y (IC50: 6 nM ). Pacritinib inhibits FLT3 phosphorylation and downstream STAT, MAPK and PI3K signaling in FLT3-internal-tandem duplication (ITD), FLT3-wt cells and primary AML blast cells. Pacritinib treatment leads to a dose-dependent decrease of pFLT3, pSTAT5, pERK1/2 and pAkt in FLT3-ITD harboring MV4-11 cells with IC50 of 80, 40, 33 and 29 nM , respectively. Treatment of the primary AML blast cells with Pacritinib for 3 h leads to a dose-dependent decrease of pFLT3, pSTAT3 and pSTAT5 with an IC50 below 0.5 μM. Pacritinib induces apoptosis, cell cycle arrest and anti-proliferative effects in FLT3-mutant and FLT3-wt cells. Pacritinib inhibits cell proliferation of FLT3-ITD-harboring cells MV4-11 (IC50: 47 nM ) and primary AML blast (IC50: 0.19-1.3 nM ) cells. Read more...
Cell Research	Cells are seeded at 30-50% confluency in 96-well plates and are treated with different concentrations of compounds (in triplicate) for 48 h. Cell viability is monitored using the CellTiter-Glo assay.(Only for Reference) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Inhibitor, Fms like tyrosine kinase 3, FLT3, FLT3 (D835Y), Janus kinase, JAK3, JAK2 (V617F), JAK, JAK2, inhibit, Pacritinib, Cluster of differentiation antigen 135, CD135, SB 1518, SB1518, SB-1518, TyrosineKinases, Tyrosine Kinases, Tyk2

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Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

46216796 ↗

Key Properties

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No computed properties available.

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CAS Number:	1228923-43-0
Formula:	C₂₈H₃₂N₄O₃.xClH

CAS Number:	1228923-42-9
MW:	664.7
Formula:	C₃₄H₄₀N₄O₁₀

MW:	480.628
Formula:	C₂₈H₂₄D₈N₄O₃

Purity:	>98%(HPLC)
CAS Number:	937272-79-2
MW:	472.6
Formula:	C₂₈H₃₂N₄O₃

Pacritinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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