Crotonoside(Synonyms: 巴豆苷; Isoguanosine)

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Crotonoside (Synonyms: 巴豆苷; Isoguanosine) 纯度: 98.18%

Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the treatment of AML.

Crotonoside(Synonyms: 巴豆苷; Isoguanosine)

Crotonoside Chemical Structure

CAS No. : 1818-71-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660 In-stock
5 mg ￥600 In-stock
10 mg ￥1000 In-stock
20 mg ￥1800 In-stock
50 mg   询价  
100 mg   询价  

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生物活性

Crotonoside is isolated from Chinese medicinal herb, Croton. Crotonoside inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. Crotonoside could be a promising new lead compound for the treatment of AML[1].

IC50 & Target[1]

FLT3

 

HDAC3

 

HDAC6

 

体外研究
(In Vitro)

Crotonoside (0-200 μM;) selectively inhibits the viability of AML cell line MV4-11, MOLM-13 (with FLT3-ITD mutant) and KG-1 (without FLT3-ITD mutant) in a dose-dependent manner with an IC50 of 11.6 μM, 12.7 μM and 17.2 μM, respectively[1].
Crotonoside (0-100μM; 7 hours) inhibits the phosphorylation of FLT3 Erk1/2, Akt/mTOR and STAT5 is strongly inhibited by crotonoside at higher concentration of 12.5 μM in a concentration-dependent manner[1].
Crotonoside (0-100 μM; 12 hours) exhibits a dose-dependent increase in the percentage of G0/G1 phase and a dose-dependent decrease in the percentage of G2/M and S phases cells[1].
Crotonoside (0-100 μM; 24 hours) leads to concentration-dependent changes in the number of apoptotic MV4-11 cells, results in a dose-dependent decrease in the level of pro-caspase-3 and a dose-dependent increase in the level of the cleaved caspase-3 fragments[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: AML cell line MV4-11, MOLM-13 and KG-1 cells
Concentration: 0-200 μM
Incubation Time: 72 hours
Result: Inhibited AML cells growth than other cell lines tested.

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM
Incubation Time: 7 hours
Result: Inhibited AML cells growth than other cell lines tested.

Cell Cycle Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM
Incubation Time: 12 hours
Result: Induced cell cycle arrest in G0/G1.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 0 μM, 12.5 μM, 25 μM, 50 μM
Incubation Time: 24 hours
Result: Induced MV4-11 cell apoptosis.

体内研究
(In Vivo)

Crotonoside(intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once daily) induces a significant antitumor activity and inhibited xenograft tumor progress as compared to treatment with vehicle[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-SCID mice with MV4-11 cells[1]
Dosage: 70 mg/kg, 35 mg/kg
Administration: Intraperitoneal and intravenous injection; 70 mg/kg, 35 mg/kg; once daily
Result: Produced significant AML tumor inhibition rates of 93.5% at 70 mg/kg.

分子量

283.24

Formula

C10H13N5O5
CAS 号

1818-71-9
中文名称

巴豆苷
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (88.26 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.5306 mL 17.6529 mL 35.3057 mL
5 mM 0.7061 mL 3.5306 mL 7.0612 mL
10 mM 0.3531 mL 1.7653 mL 3.5306 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。-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 (7.34 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.34 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% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.34 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.34 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 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: ≥ 2.08 mg/mL (7.34 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.34 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]. Li YZ,et al. Crotonoside exhibits selective post-inhibition effect in AML cells via inhibition of FLT3 and HDAC3/6. Oncotarget. 2017 Sep 8;8(61):103087-103099.

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