Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC₅₀s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

IC50: 1 nM (Tie-2), 35 nM (p38α), 26 nM (p38β)^[1]

Pexmetinib is a Tie-2 and p38 MAPK dual inhibitor, with IC₅₀s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively. Pexmetinib also shows IC₅₀s of 4 nM (Abl), 10 nM (Arg), 28 nM (FGFR1), 47 nM (Flt1), 42 nM (Flt4), 41 nM (Fyn), 26 nM (Hck), 25 nM (Lyn), and 26 nM (MINK), respectively. Pexmetinib (0.5, 1 μM) blocks leukemic cell proliferation and stimulates hematopoietic activity in myelodysplastic syndromes^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

556.63

C₃₁H₃₃FN₆O₃

945614-12-0

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 125 mg/mL (224.57 mM)

* “≥” means soluble, but saturation unknown.

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.74 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.74 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (3.74 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (3.74 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Bachegowda L, et al. Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer Res. 2016 Aug 15;76(16):4841-4849.

Cell lines and primary samples are incubated at indicated doses of of TIE2/p38 inhibitor Pexmetinib. Viability is assessed by addition of Cell Titer Blue and measured via Fluostar Omega Microplate reader^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Bachegowda L, et al. Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer Res. 2016 Aug 15;76(16):4841-4849.