1G244|cas:847928-32-9|西域试剂

1G244,98.66%

产品编号：Bellancom-116304| CAS NO：847928-32-9| 分子式：C₂₉H₃₀F₂N₄O₂| 分子量：504.57

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货号	价格	库存与货期
Bellancom-116304	￥700.00	杭州北京（现货）
Bellancom-116304	￥1120.00	杭州北京（现货）
Bellancom-116304	￥2240.00	杭州北京（现货）
Bellancom-116304	￥3580.00	杭州北京（现货）
Bellancom-116304	￥5730.00	杭州北京（现货）

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1G244

产品介绍

1G244 是一种有效的 DPP8/9 抑制剂，IC₅₀ 分别为 12 nM 和 84 nM，但不抑制 DPPIV 和 DPPII。1G244 可诱导多发性骨髓瘤细胞凋亡，并具有抗骨髓瘤作用。

生物活性

1G244 is a potent DPP8/9 inhibitor with IC₅₀s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects.

体外研究

1G244 (0-100 μM; 72 hours; Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells) treatment dose-dependently decreases viable cell number of five multiple myeloma cell lines.
1G244 (50 μM; 0-48 hours; MM.1 S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected.

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

Cell Viability Assay

Cell Line:	Delta47, U266 , KMS-5, RPMI8226, or MM.1 S cells
Concentration:	0 μM, 1 μM, 5 μM, 10 μM, 50 μM, or 100 μM
Incubation Time:	72 hours
Result:	Dose-dependently decreased viable cell number of five multiple myeloma cell lines.

Western Blot Analysis

Cell Line:	MM.1 S cells
Concentration:	50 μM
Incubation Time:	0 hour, 3 hours, 6 hours, 12 hours, 24 hours, 48 hours
Result:	Decreased caspase-3 and PARP protein.

体内研究
(In Vivo)

1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model.

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

Animal Model:	NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells
Dosage:	30 mg/kg
Administration:	Subcutaneous injection; once-a-week; for 3 weeks
Result:	Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model.

体内研究

1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model.

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

Animal Model:	NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells
Dosage:	30 mg/kg
Administration:	Subcutaneous injection; once-a-week; for 3 weeks
Result:	Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model.

体内研究

1G244 (30 mg/kg; subcutaneous injection; once-a-week; for 3 weeks; NOG female mice) treatment apparently suppresses the subcutaneous growth of MM.1 S cells in murine xenograft model.

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

Animal Model:	NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells
Dosage:	30 mg/kg
Administration:	Subcutaneous injection; once-a-week; for 3 weeks
Result:	Apparently suppressed the subcutaneous growth of MM.1 S cells in murine xenograft model.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (495.47 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9819 mL	9.9094 mL	19.8189 mL
5 mM	0.3964 mL	1.9819 mL	3.9638 mL
10 mM	0.1982 mL	0.9909 mL	1.9819 mL

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 (sealed storage, away from moisture and light)。-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: ≥ 2.08 mg/mL (4.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.12 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% corn oil
Solubility: ≥ 2.08 mg/mL (4.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.12 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。