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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-Pacritinib
Pacritinib

Chemical Structure : Pacritinib

CAS No.: 937272-79-2

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Pacritinib (SB1518)

货号: PC-22993Not For Human Use, Lab Use Only.

Pacritinib (SB1518) is a potent, selective JAK2/FLT3 inhibitor with IC50 of 23 and 19 nM for JAK2(WT) and JAK2(V617F), and IC50 of 22 nM for FLT3.

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5 mg ￥1180 In stock
10 mg ￥1980 In stock
25 mg ￥3580 In stock
50 mg ￥5580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Pacritinib (SB1518) is a potent, selective JAK2/FLT3 inhibitor with IC50 of 23 and 19 nM for JAK2(WT) and JAK2(V617F), and IC50 of 22 nM for FLT3.
Pacritinib (SB1518) selectivity against JAK1 and JAK3 (IC(50) = 1280 and 520 nM, respectively).
Pacritinib (SB1518) shows potent effects on cellular JAK/STAT pathways, inhibiting tyrosine phosphorylation on JAK2 (Y221) and downstream STATs.
Pacritinib (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.
Pacritinib (SB1518) significantly reduces splenomegaly and hepatomegaly in a JAK2(V617F)-driven disease model.
Pacritinib (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.

物理化学性质&存储条件

分子量 472.59
分子式 C28H32N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(16E)-11-[2-(1-Pyrrolidinyl)ethoxy]-14,19-dioxa-5,7,27-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene

参考文献

1. Hart S, et al. Blood Cancer J. 2011 Nov;1(11):e44.

2. William AD, et al. J Med Chem. 2011 Jul 14;54(13):4638-58.

3. Hart S, et al. Leukemia. 2011 Nov;25(11):1751-9.

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