AG-270|cas:2201056-66-6|西域试剂

AG-270,99.58%

产品编号：Bellancom-138630| CAS NO：2201056-66-6| 分子式：C₃₀H₂₇N₅O₂| 分子量：489.57

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货号	价格	库存与货期
Bellancom-138630	￥3000.00	杭州北京（现货）
Bellancom-138630	￥4800.00	杭州北京（现货）
Bellancom-138630	￥8800.00	杭州北京（现货）
Bellancom-138630	￥14000.00	杭州北京（现货）

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AG-270

产品介绍

AG-270 是非竞争性的、首创的、可逆的、具有口服活性的 MAT2A 变构抑制剂，其 IC₅₀ 值为 14 nM。

生物活性

AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC₅₀ of 14 nM.

体外研究

AG-270 demonstrates potent reduction in levels of intracellular SAM, as well as MTAP-null–selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro.
AG-270 exhibits an IC₅₀ of 20 nM in HCT116 MTAP-null cell SAM at 72 h.
MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.
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%.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Pancreatic KP4 MTAP-null xenograft mouse model.
Dosage:	10-200 mg/kg.
Administration:	Orally, q.d. for 38 days.
Result:	Led to dose-dependent reductions in tumor SAM levels and tumor growth of KP4 MTAP-null xenografts (TGI = 36% (10 mg/kg), 48% (30 mg/kg), 66% (100 mg/kg), 67% (200 mg/kg).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Pancreatic KP4 MTAP-null xenograft mouse model.
Dosage:	10-200 mg/kg.
Administration:	Orally, q.d. for 38 days.
Result:	Led to dose-dependent reductions in tumor SAM levels and tumor growth of KP4 MTAP-null xenografts (TGI = 36% (10 mg/kg), 48% (30 mg/kg), 66% (100 mg/kg), 67% (200 mg/kg).

性状

Solid

溶解性数据

In Vitro:

DMSO : 4 mg/mL (8.17 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0426 mL	10.2130 mL	20.4261 mL
5 mM	0.4085 mL	2.0426 mL	4.0852 mL
10 mM	---	---	---

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: ≥ 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-CD in 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 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