MT-DADMe-ImmA is an inhibitor of human 5′-methylthioadenosine phosphorylase (MTAP) with a K_i of 90 pM.

Ki: 90 pM (MTAP)^[1]

Treatment of cultured cells with MT-DADMe-ImmA and MTA inhibit MTAP, increase cellular MTA concentrations, decrease polyamines, and induce apoptosis in FaDu and Cal27, two head and neck squamous cell carcinoma cell lines. The same treatment does not induce apoptosis in normal human fibroblast cell lines (CRL2522 and GM02037) or in MCF7, a breast cancer cell line with an MTAP gene deletion. MT-DADMe-ImmA alone does not induce apoptosis in any cell line, implicating MTA as the active agent^[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.

The t_1/2 for onset of inhibition is 50 min with complete inhibition by 250 min. MTAP activity slowly returns, giving a biological half-life for the action of oral MT-DADMe-ImmA of 6.3 days. The time-dependent growth of FaDu tumors in immunodeficient mice is suppressed by oral or intraperitoneal treatment with MT-DADMe-ImmA^[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.

293.39

C₁₃H₁₉N₅OS

653592-04-2

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 : 100 mg/mL (340.84 mM; Need ultrasonic)

*

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 (8.52 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.52 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 (8.52 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.52 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 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 (8.52 mM); Clear solution

  此方案可获得 ≥ 2.5 mg/mL (8.52 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]. Evans GB, et al. Second generation transition state analogue inhibitors of human 5′-methylthioadenosine phosphorylase. J Med Chem. 2005 Jul 14;48(14):4679-89.

  [2]. Basu I, et al. A transition state analogue of 5′-methylthioadenosine phosphorylase induces apoptosis in head and neck cancers. J Biol Chem. 2007 Jul 20;282(29):21477-86.

Cell viability is evaluated using the Alamar Blue assay. Cells are seeded onto 96-well plates at a density of 104 cells/well and incubated with increasing concentrations of MT-DADMe-ImmA (100 pM to 100 μM) for 4 days at fixed MTA concentrations (0, 5, 10, and 20 μM). IC₅₀ is determined with the assay data^[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.

Mice: Tumors were established in mice for 5 days prior to oral or intraperitoneal treatments with MT-DADMe-ImmA. Mice are treated with oral dose of 21 mg/kg or an intraperitoneal dose of 5 mg/kg/day MT-DADMe-ImmA^[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]. Evans GB, et al. Second generation transition state analogue inhibitors of human 5′-methylthioadenosine phosphorylase. J Med Chem. 2005 Jul 14;48(14):4679-89.

  [2]. Basu I, et al. A transition state analogue of 5′-methylthioadenosine phosphorylase induces apoptosis in head and neck cancers. J Biol Chem. 2007 Jul 20;282(29):21477-86.