Crotonoside
(Synonyms: 巴豆苷; Isoguanosine) 目录号 : GC38412
Crotonoside是一种FLT3和HDAC3/6抑制剂，可用于研究急性髓系白血病(AML)。
Cas No.:1818-71-9
Sample solution is provided at 25 µL, 10mM.
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Crotonoside is a FLT3 and HDAC3/6 inhibitor that can be used to study acute myeloid leukemia (AML)[1].
Crotonoside (50μM, 24h) induced late apoptosis in about 50% AML cell line MV4-11[1]. Crotonoside (7.5, 15, or 30μM; 48h) significantly induced AML cell apoptosis in a dose-dependent manner[2].
Crotonoside (25, 50, or 100mg/kg; 20 days; i.p.) ameliorated the severity of collagen-induced arthritis (CIA) in mice[3]. Compared with the rabbits in the normal saline (NS) group, the group given Crotonoside (4.5mg/kg, intravenous injection) effectively prolonged the time of aconitine-induced arrhythmias and significantly reduced the incidence of ventricular tachycardia (VT) and ventricular fibrillation (VF)[4].
References:
[1] Li YZ, Yu S, Yan PA, et al. Crotonoside exhibits selective post-inhibition effect in AML cells via inhibition of FLT3 and HDAC3/6. Oncotarget. 2017 Nov 11;8(61):103087.
[2] Ma C, Liu P, Cui S, et al. The identification of APOBEC3G as a potential prognostic biomarker in acute myeloid leukemia and a possible drug target for crotonoside. Molecules. 2022 Sep 7;27(18):5804.
[3] Lin SC, Lin CC, Li S, et al. Alleviation of collagen-induced arthritis by crotonoside through modulation of dendritic cell differentiation and activation. Plants. 2020 Nov 10;9(11):1535.
[4] Liu Z, Jia Y, Song L, et al. Antiarrhythmic effect of crotonoside by regulating sodium and calcium channels in rabbit ventricular myocytes. Life sciences. 2020 Mar 1;244:117333.
Crotonoside是一种FLT3和HDAC3/6抑制剂，可用于研究急性髓系白血病(AML)[1]。
Crotonoside（50μM，24小时）诱导约50%的AML细胞株MV4-11发生晚期凋亡[1]。Crotonoside（7.5、15或30μM，48小时）以剂量依赖性方式显著诱导AML细胞凋亡[2]。
Crotonoside（25、50或100 mg/kg，20天，腹腔注射）可改善小鼠胶原诱导性关节炎（CIA）的严重程度[3]。与生理盐水（NS）组的兔相比，Crotonoside（4.5mg/kg，静脉注射）组能有效延长Crotonoside诱发的心律失常时间，并明显降低室性心动过速（VT）和心室颤动（VF）的发生率[4]。
| Cell experiment [1]: | |
|
Cell lines |
Acute myeloid leukemia (AML) cell line MV4-11 |
|
Preparation Method |
MV4-11 cells were treated with Crotonoside (25, 50, and 100μM) or 0.1% DMSO for 24 hours. After treatment MV4-11 cells were harvested, washed with PBS and stained for apoptosis using the Annexin V-fluorescein isothiocyanate (FITC) Apoptosis Detection Kit. |
|
Reaction Conditions |
25, 50, and 100μM; 16 or 24 hours |
|
Applications |
Crotonoside (50μM, 24h) induced late apoptosis in about 50% AML cells. |
| Animal experiment [2]: | |
|
Animal models |
Collagen-induced arthritic (CIA) mouse model |
|
Preparation Method |
Crotonoside was dissolved in a solvent of 10% DMSO and 90% glyceryl trioctanoate. The mice were randomly divided into four groups (n = 6 per group), including normal, CIA vehicle control, Methotrexate (MTX)-treated and Crotonoside-treated mice at 25, 50, or 100mg/kg. MTX (0.5mg/kg) and Crotonoside treatments were intraperitoneally administered once daily from day 21 to day 41 after the first immunization, whereas vehicle control mice received the solvent. |
|
Dosage form |
25, 50, or 100mg/kg; 20 days; i.p. |
|
Applications |
Crotonoside ameliorated the severity of collagen-induced arthritis (CIA) in mice. |
|
References: |
|
| Cas No. | 1818-71-9 | SDF | |
| 别名 | 巴豆苷; Isoguanosine | ||
| Canonical SMILES | OC[C@@H]1[C@H]([C@H]([C@H](N2C=NC(C(N)=N3)=C2NC3=O)O1)O)O | ||
| 分子式 | C10H13N5O5 | 分子量 | 283.24 |
| 溶解度 | DMSO: 25 mg/mL (88.26 mM) | 储存条件 | Store at -20°C,protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 | 7.0611 mL |
| 10 mM | 0.3531 mL | 1.7653 mL | 3.5306 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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