AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally activeMAT2Ainhibitor, with anIC₅₀of 14 nM^[1].

IC50: 14 nM (MAT2A)^[1].

AG-270 demonstrates potent reduction in levels of intracellularSAM, as well as MTAP-null–selective antiproliferative activity in the HCT116 MTAP isogenic cell modelin vitro^[1].
AG-270 exhibits an IC₅₀of 20 nM in HCT116 MTAP-null cell SAM at 72 h^[1].
MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM)^[2].

AG-270 shows excellent microsomal, hepatocyte, and in vivo metabolic stability across species (human, mouse, rat, dog, and monkey). AG-270 exhibits T1/2 values of 5.9 h, 4.2 h, 4.8 h and 21.3 h in mouse, rat, monkey and dog, respectively^[1].
AG-270 (200 mg/kg, orally, q.d. for 38 days) results in dose-dependent reduction in tumor SAM levels and tumor growth of KP4 MTAP-null xenografts and is well tolerated, with mean body weight loss<5%^[1].
Combining AG-270 with taxanes and gemcitabine yielded additive-tosynergistic antitumor activity, with the docetaxel combination yielding 50% complete tumor regressions in select models; combination benefits are observed in PDX models derived from esophageal, NSCLC, and pancreatic cancers^[2].

489.57

Solid

C₃₀H₂₇N₅O₂

2201056-66-6

Room temperature in continental US; may vary elsewhere.

DMSO : 8.33 mg/mL(17.01 mM;ultrasonic and warming and heat to 60℃)

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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: ≥ 4.75 mg/mL (9.70 mM); Clear solution

  此方案可获得 ≥ 4.75 mg/mL (9.70 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 47.5 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-CDin saline)

  Solubility: ≥ 4.75 mg/mL (9.70 mM); Clear solution

  此方案可获得 ≥ 4.75 mg/mL (9.70 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 47.5 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 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