1G244

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1G244  纯度: 98.55%

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。

1G244

1G244 Chemical Structure

CAS No. : 847928-32-9

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1G244 相关产品

•相关化合物库:

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  • Apoptosis Compound Library
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  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library

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[1][2].

IC50 & Target

IC50: 12 nM (DPP8), 84 nM (DPP9)[2]
体外研究
(In Vitro)

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[1].
1G244 (50 μM; 0-48 hours; MM.1 S cells) treatment induces apoptosis, as cleaved forms of both caspase-3 and PARP are detected[1].

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.

Cell Viability Assay[1]

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[1]

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[1].

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.

Animal Model: NOD/Shi-scid IL-2Rγnull (NOG) female mice (6-7 weeks; 19-21 g) injected with MM.1 S cells[1]
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.

分子量

504.57

Formula

C29H30F2N4O2
CAS 号

847928-32-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Sato T, et al. DPP8 is a novel therapeutic target for multiple myeloma. Sci Rep. 2019 Dec 2;9(1):18094.

    [2]. Leen Heirbaut, et al. Probing for improved selectivity with dipeptidederived inhibitors of dipeptidyl peptidases 8 and 9: the impact of P1-variation. MedChemComm. 2016, 7.

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