Pacritinib|cas 937272-79-2|DC Chemicals|Price|Buy

Cas No.:	937272-79-2
Chemical Name:	Pacritinib (SB1518)
Synonyms:	SB1518; SB 1518; SB-1518
SMILES:	C1(COC/C=C/COCC2=C(OCCN3CCCC3)C=CC4=C2)=CC=CC(C5=N/C(NC=C5)=N4)=C1
Formula:	C₂₈H₃₂N₄O₃
M.Wt:	472.58
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Pacritinib (SB1518) is a potent and selective JAK2 (IC50 = 23 and 19 nM For JAK2(WT) and JAK2(V617F), respectively) and FLT3 (IC(50) = 22 nM) inhibitor with selectivity against JAK1 and JAK3 (IC(50) = 1280 and 520 nM, respectively). IC50 Value: 23 nM (JAK2 wt); 22 nM (FLT3) Target: JAK2; FLT3 in vitro: SB1518 shows potent effects on cellular JAK/STAT pathways, inhibiting tyrosine phosphorylation on JAK2 (Y221) and downstream STATs. As a consequence SB1518 has potent anti-proliferative effects on myeloid and lymphoid cell lines driven by mutant or wild-type JAK2 or FLT3, resulting from cell cycle arrest and induction of apoptosis . in vivo: SB1518 has favorable pharmacokinetic properties after oral dosing in mice, is well tolerated and significantly reduces splenomegaly and hepatomegaly in a JAK2(V617F)-driven disease model. SB1518 dose-dependently inhibits intra-tumor JAK2/STAT5 signaling, leading to tumor growth inhibition in a subcutaneous model generated with SET-2 cells derived from a JAK2(V617F) patient with megakaryoblastic leukemia . Oral administration of pacritinib in murine models of FLT3-ITD-driven AML led to significant inhibition of primary tumor growth and lung metastasis. Upregulation of JAK2 in FLT3-TKI-resistant AML cells was identified as a potential mechanism of resistance to selective FLT3 inhibition . Pracinostat and pacritinib in combination showed synergy on tumor growth, reduction of metastases and synergistically decreased JAK2 or FLT signaling, depending on the cellular context .For the detailed information of Pacritinib, the solubility of Pacritinib in water, the solubility of Pacritinib in DMSO, the solubility of Pacritinib in PBS buffer, the animal experiment (test) of Pacritinib, the cell expriment (test) of Pacritinib, the in vivo, in vitro and clinical trial test of Pacritinib, the EC50, IC50,and Affinity of Pacritinib, Please contact DC Chemicals.

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2018-0101

Cat. No.	Product name	Field of application
DC47590	Ten01	Ten01 has 5.0 nM activity against JAK1 kinase.
DC47041	Lorpucitinib	Lorpucitinib is a Gut-Restricted JAK Inhibitor for the research of Inflammatory Bowel Disease.
DC47039	Itacnosertib	Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871.
DC46857	Nezulcitinib	Nezulcitinib (TD-0903) is an inhaled and lung-selective pan-Janus kinase (JAK) inhibitor. Nezulcitinib can be used for the research of COVID-19 associated acute lung injury and impaired oxygenation.
DC46856	JAK2/FLT3-IN-1 TFA	JAK2/FLT3-IN-1 (TFA) is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.
DC46855	Deuruxolitinib	Deuruxolitinib (CTP-543), a deuterated Ruxolitinib, modulates the activity of JAK1/JAK2. Deuruxolitinib can be used for the research hair loss disorders (from patent WO2017192905A1, compound I).
DC44160	JAK2/FLT3-IN-1	JAK2/FLT3-IN-1 is a potent and orally active dual JAK2/FLT3 inhibitor with IC50 values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.
DC42325	(3S,4S)-Tofacitinib	(3S,4S)-Tofacitinib is the less active S-enantiomer of Tofacitinib. Tofacitinib inhibits JAK3 with IC50 of 1 nM.
DC42324	JAK2-IN-7	JAK2-IN-7 is a selective JAK2 with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.
DC41406	Coumermycin A1	Coumermycin A1 is a JAK2 signal activator. Coumermycin A1 inhibits DNA Gyrase which thereby inhibits cell division in bacteria.