货号	规格	价格	上海	北京	珠海	重庆	武汉
S81134-5mg促销	≥95%	￥925.00 ￥832.00 S81134-5mg ￥832.00 现货	10 0 10	-	-	-	-
S81134-10mg促销	≥95%	￥1570.00 ￥1413.00 S81134-10mg ￥1413.00 现货	10 10	-	-	-	-
S81134-25mg促销	≥95%	￥2770.00 ￥2493.00 S81134-25mg ￥2493.00 现货	6 6	-	-	-	-
S81134-50mg促销	≥95%	￥4634.00 ￥4170.00 S81134-50mg ￥4170.00 现货	2 2	-	-	-	-

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产品描述：

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).

靶点：

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);FLT; TyrosineKinases; JAK

体内研究：

For evaluation of efficacy in the Ba/F3-JAK2V617F 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. In rats, Pacritinib (SB1518) shows moderately fast absorption (tmax=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 (tmax=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

参考文献：

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. 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. 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

溶解性：

Soluble in DMSO

保存条件：

2-8℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.116 ml	10.58 ml	21.16 ml
5 mM	0.423 ml	2.116 ml	4.232 ml
10 mM	0.212 ml	1.058 ml	2.116 ml
50 mM	0.042 ml	0.212 ml	0.423 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

帕克替尼（SB1518）

Pacritinib

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)