ZM 336372 is a potent inhibitor of the protein kinase c-Raf. The IC₅₀ value is 0.07 μM in the standard assay, which contains 0.1 mM ATP.

ZM 336372 is a potent inhibitor of human c-Raf. The IC₅₀ value is 0.07 μM in the standard assay, which contains 0.1 mM ATP. The IC₅₀, decreases to 0.01μM at 0.025 mM ATP and increases to 0.9 μM at 2.5 mM ATP indicating that ZM 336372 is a competitive inhibitor with respect to ATP. ZM 336372 inhibits c-Raf tenfold more potently than B-Raf^[1]. Cell proliferation analysis of ZM336372. 3,4-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide growth assay of H727 and BON treated as control, DMSO, and 100 μM ZM336372 to days 16 and 10, respectively. Both H727 and BON cell proliferation is inhibited in the presence of drug compared with controls. H727 cells treated with ZM336372 are growth suppressed, whereas control treatments have significantly more growth by day 6, continuing up to 16 days. A similar response is also seen in BON cells as growth suppression occurred as early as day 4 and was maintained out to day 10^[2].

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.

389.45

C₂₃H₂₃N₃O₃

208260-29-1

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 50 mg/mL (128.39 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

*

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。

In Vivo:

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: ≥ 2.5 mg/mL (6.42 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.42 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 25.0 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: 2.5 mg/mL (6.42 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.5 mg/mL (6.42 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (6.42 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (6.42 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Hall-Jackson CA, et al. Paradoxical activation of Raf by a novel Raf inhibitor. Chem Biol. 1999 Aug;6(8):559-68.

  [2]. Van Gompel JJ, et al. ZM336372, a Raf-1 activator, suppresses growth and neuroendocrine hormone levels in carcinoid tumor cells. Mol Cancer Ther. 2005 Jun;4(6):910-7.

Proliferation of H727 and BON cells after treatment with ZM336372 is measured using a 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide. Cells are trypsinized and plated in triplicate to 24-well plates and allowed to adhere overnight. Then, cells are treated with either 100 μM ZM336372 or DMSO (2%) and incubated. Media are changed every 2 days with new treatment. At each time point, cell growth rates are analyzed after the addition of 3,4-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide reagent to the cultured cells. Absorbance is determined using spectrophotometer at a wavelength of 540 nm^[2].

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]. Hall-Jackson CA, et al. Paradoxical activation of Raf by a novel Raf inhibitor. Chem Biol. 1999 Aug;6(8):559-68.

  [2]. Van Gompel JJ, et al. ZM336372, a Raf-1 activator, suppresses growth and neuroendocrine hormone levels in carcinoid tumor cells. Mol Cancer Ther. 2005 Jun;4(6):910-7.