 
        
        
        
                货号:A508462
                
                同义名:
                    
                        
                            巴豆苷(异鸟苷)
                            
                             / Isoguanosine; 2-Hydroxyadenosine
                            
                        
                    
                
                
                
                    
                     
                
            
Crotonoside 是从中草药巴豆(Croton tiglium)中分离出的。Crotonoside 抑制 FLT3 和 HDAC3/6,在急性髓性白血病(AML)细胞中表现出选择性的抑制作用。Crotonoside 可能是 AML 研究中有前途的新先导化合物。
 
                                 
                                
                            

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| 产品名称 | HD1 ↓ ↑ | HD2 ↓ ↑ | HDAC ↓ ↑ | HDAC1 ↓ ↑ | HDAC10 ↓ ↑ | HDAC11 ↓ ↑ | HDAC2 ↓ ↑ | HDAC3 ↓ ↑ | HDAC4 ↓ ↑ | HDAC5 ↓ ↑ | HDAC6 ↓ ↑ | HDAC7 ↓ ↑ | HDAC8 ↓ ↑ | HDAC9 ↓ ↑ | 其他靶点 | 纯度 | |||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Givinostat HCl monohydrate | ++++ HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM | +++ HD2, IC50: 10 nM | 99%+ | ||||||||||||||||
| MC1568 | ++ HD1-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM | 96% | |||||||||||||||||
| Trichostatin A | ++++ HDAC, IC50: ~1.8 nM | 99%+ | |||||||||||||||||
| Scriptaid | ✔ | 99%+ | |||||||||||||||||
| Valproic acid sodium | ✔ | Autophagy | 97% | ||||||||||||||||
| AR-42 | +++ HDAC, IC50: 30 nM | 99%+ | |||||||||||||||||
| Dacinostat | +++ HDAC, IC50: 32 nM | 98+% | |||||||||||||||||
| CUDC-101 | ++++ HDAC, IC50: 4.4 nM | ++++ HDAC1, IC50: 4.5 nM | +++ HDAC10, IC50: 26.1 nM | +++ HDAC2, IC50: 12.6 nM | ++++ HDAC3, IC50: 9.1 nM | +++ HDAC4, IC50: 13.2 nM | +++ HDAC5, IC50: 11.4 nM | ++++ HDAC6, IC50: 5.1 nM | + HDAC7, IC50: 373 nM | ++ HDAC8, IC50: 79.8 nM | ++ HDAC9, IC50: 67.2 nM | EGFR,HER2 | 99%+ | ||||||
| M344 | ++ HDAC, IC50: 100 nM | 99%+ | |||||||||||||||||
| Splitomicin | + Sir2p, IC50: 60 μM | 99% | |||||||||||||||||
| Panobinostat | ++++ HDAC (MOLT-4 cells), IC50: 5 nM HDAC (Reh cells), IC50: 20 nM | 98% | |||||||||||||||||
| Sodium 4-Phenylbutyrate | ✔ | 98% | |||||||||||||||||
| Vorinostat | +++ HDAC, IC50: ~10 nM | 98% | |||||||||||||||||
| Curcumin | ✔ | Nrf2,NF-κB | 98% | ||||||||||||||||
| Belinostat | +++ HDAC, IC50: 27 nM | 98% | |||||||||||||||||
| RG-2833 | ++ HDAC1, Ki: 32 nM | ++ HDAC3, Ki: 5 nM | 98% | ||||||||||||||||
| Valproic acid | + HDAC1, IC50: 0.4 mM | 98% | |||||||||||||||||
| BG45 | + HDAC1, IC50: 2 μM | + HDAC2, IC50: 2.2 μM | + HDAC3, IC50: 289 nM | 99%+ | |||||||||||||||
| Entinostat | + HDAC1, IC50: 0.51 μM | + HDAC3, IC50: 1.7 μM | 98% | ||||||||||||||||
| Resminostat | +++ HDAC1, IC50: 42.5 nM | ++ HDAC3, IC50: 50.1 nM | ++ HDAC6, IC50: 71.8 nM | 98+% | |||||||||||||||
| Romidepsin | +++ HDAC1, IC50: 36 nM | +++ HDAC2, IC50: 47 nM | 99%+ | ||||||||||||||||
| Parthenolide | ✔ | p53,NF-κB | 97% HPLC | ||||||||||||||||
| Tacedinaline | + HDAC1, IC50: 0.9 μM | + HDAC2, IC50: 0.9 μM | + HDAC3, IC50: 1.2 μM | 98% | |||||||||||||||
| Mocetinostat | ++ HDAC1, IC50: 0.15 μM | + HDAC11, IC50: 0.59 μM | + HDAC2, IC50: 0.29 μM | + HDAC3, IC50: 1.66 μM | 98% | ||||||||||||||
| WT-161 | ++++ HDAC1, IC50: 8.35 nM | +++ HDAC2, IC50: 15.4 nM | ++++ HDAC6, IC50: 0.4 nM | 99%+ | |||||||||||||||
| Fimepinostat | ++++ HDAC1, IC50: 1.7 nM | ++++ HDAC10, IC50: 2.8 nM | ++++ HDAC11, IC50: 5.4 nM | ++++ HDAC2, IC50: 5.0 nM | ++++ HDAC3, IC50: 1.8 nM | +++ HDAC6, IC50: 27 nM | 99%+ | ||||||||||||
| Tucidinostat | ++ HDAC1, IC50: 95 nM | ++ HDAC10, IC50: 78 nM | ++ HDAC2, IC50: 160 nM | ++ HDAC3, IC50: 67 nM | 99%+ | ||||||||||||||
| Santacruzamate A | ++++ HDAC2, IC50: 119 pM | 99%+ | |||||||||||||||||
| (E,E)-RGFP966 | ++ HDAC3, IC50: 80 nM | 99%+ | |||||||||||||||||
| LMK-235 | +++ HDAC4, IC50: 11.9 nM | ++++ HDAC5, IC50: 4.2 nM | 99%+ | ||||||||||||||||
| Tasquinimod | ✔ | 99%+ | |||||||||||||||||
| CAY10603 | ++++ HDAC6, IC50: 2 pM | 98% | |||||||||||||||||
| Tubastatin A | +++ HDAC6, IC50: 15 nM | 98% | |||||||||||||||||
| Tubacin | ++++ HDAC6, IC50: 4 nM | 99%+ | |||||||||||||||||
| ACY-738 | ++++ HDAC6, IC50: 1.7 nM | 99%+ | |||||||||||||||||
| Nexturastat A | ++++ HDAC6, IC50: 5 nM | 99%+ | |||||||||||||||||
| BRD73954 | +++ HDAC6, IC50: 36 nM | ++ HDAC8, IC50: 120 nM | 99% | ||||||||||||||||
| Tubastatin A HCl | +++ HDAC6, IC50: 15 nM | + HDAC8, IC50: 854 nM | 98% | ||||||||||||||||
| PCI-34051 | +++ HDAC8, IC50: 10 nM | 99%+ | |||||||||||||||||
| Ricolinostat | ++ HDAC1, IC50: 58 nM | ++ HDAC2, IC50: 48 nM | ++ HDAC3, IC50: 51 nM | ++++ HDAC6, IC50: 4.7 nM | ++ HDAC8, IC50: 100 nM | 99%+ | |||||||||||||
| Droxinostat | + HDAC3, IC50: 16.9 μM | + HDAC6, IC50: 2.47 μM | + HDAC8, IC50: 1.46 μM | 99%+ | |||||||||||||||
| Abexinostat | ++++ HDAC1, Ki: 7 nM | +++ HDAC10, IC50: 24 nM | +++ HDAC2, Ki: 19 nM | ++++ HDAC3/SMRT, Ki: 8.2 nM | +++ HDAC6, Ki: 17 nM | + HDAC8, IC50: 280 nM | 98%+ | ||||||||||||
| Citarinostat | +++ HDAC1, IC50: 35 nM | +++ HDAC2, IC50: 45 nM | +++ HDAC3, IC50: 46 nM | ++++ HDAC6, IC50: 2.6 nM | ++ HDAC8, IC50: 137 nM | 99%+ | |||||||||||||
| HPOB | + HDAC1, IC50: 2.9 μM | + HDAC10, IC50: 3.0 μM | + HDAC2, IC50: 4.4 μM | + HDAC3, IC50: 1.7 μM | ++ HDAC6, IC50: 56 nM | + HDAC8, IC50: 2.8 μM | 97% | ||||||||||||
| Quisinostat 2HCl | ++++ HDAC1, IC50: 0.11 nM | ++++ HDAC10, IC50: 0.46 nM | ++++ HDAC11, IC50: 0.37 nM | ++++ HDAC2, IC50: 0.33 nM | ++++ HDAC3, IC50: 4.86 nM | ++++ HDAC4, IC50: 0.64 nM | ++++ HDAC5, IC50: 3.69 nM | ++++ HDAC8, IC50: 4.26 nM | 97% | ||||||||||
| Domatinostat | + HDAC1, IC50: 1.20 μM | + HDAC10, IC50: 21 μM | + HDAC11, IC50: 9.7 μM | + HDAC2, IC50: 1.12 μM | + HDAC3, IC50: 0.57 μM | + HDAC5, IC50: 11.3 μM | + HDAC9, IC50: 50 μM | 99%+ | |||||||||||
| TMP269 | ++ HDAC4, IC50: 157 nM | ++ HDAC5, IC50: 97 nM | +++ HDAC7, IC50: 43 nM | +++ HDAC9, IC50: 23 nM | 99%+ | ||||||||||||||
| Pracinostat | ++ HDAC1, IC50: 49 nM | +++ HDAC10, IC50: 40 nM | ++ HDAC11, IC50: 93 nM | ++ HDAC2, IC50: 96 nM | +++ HDAC3, IC50: 43 nM | ++ HDAC4, IC50: 56 nM | +++ HDAC5, IC50: 47 nM | + HDAC6, IC50: 1.008 μM | ++ HDAC7, IC50: 137 nM | ++ HDAC8, IC50: 140 nM | ++ HDAC9, IC50: 70 nM | 99%+ | |||||||
| TMP195 | ++ HDAC4, Ki: 59 nM | ++ HDAC5, Ki: 60 nM | +++ HDAC7, Ki: 26 nM | +++ HDAC9, Ki: 15 nM | 99%+ | ||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 产品名称 | FLT3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| R406 | ✔ | Syk | 98% | ||||||||||||||||
| Go6976 | ✔ | 99%+ | |||||||||||||||||
| Quizartinib | +++ FLT3 (WT), IC50: 4.2 nM FLT3 (ITD), IC50: 1.1 nM | 98% | |||||||||||||||||
| Gilteritinib | ++++ FLT3, IC50: 0.29 nM | 99%+ | |||||||||||||||||
| Amuvatinib | + FLT3 (D835Y), IC50: 81 nM | 99%+ | |||||||||||||||||
| Pacritinib | ++ FLT3, IC50: 22 nM FLT3 (D835Y), IC50: 6 nM | 97% | |||||||||||||||||
| Dovitinib | ++++ FLT3, IC50: 1 nM | c-Kit | 99%+ | ||||||||||||||||
| Denfivontinib | ++++ FLT3, IC50: 0.4 nM FLT3 (D835Y), IC50: 0.4 nM | RET | 99%+ | ||||||||||||||||
| TAK-659 HCl | ++ FLT3, IC50: 4.6 nM | Syk | 99%+ | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | Crotonoside is isolated from Chinese medicinal herb, Croton and inhibits FLT3 and HDAC3/6, exhibits selective inhibition in acute myeloid leukemia (AML) cells. In vivo, crotonoside treatment at 70 and 35 mg/kg/d produced significant AML tumor inhibition rates of 93.5% and 73.6%, respectively. 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. Crotonoside (0 – 100 μM; 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. 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[3]. | 
| 计算器 | ||||
| 存储液制备 |  | 1mg | 5mg | 10mg | 
| 1 mM 5 mM 10 mM | 3.53mL 0.71mL 0.35mL | 17.65mL 3.53mL 1.77mL | 35.31mL 7.06mL 3.53mL | |
| CAS号 | 1818-71-9 | 
| 分子式 | C10H13N5O5 | 
| 分子量 | 283.24 | 
| SMILES Code | OC[C@@H]1[C@H]([C@H]([C@H](N2C=NC3=C2N=C(O)N=C3N)O1)O)O | 
| MDL No. | MFCD04971989 | 
| 别名 | 巴豆苷(异鸟苷) ;Isoguanosine; 2-Hydroxyadenosine; NSC 12161; Isoguanine riboside | 
| 运输 | 蓝冰 | 
| InChI Key | MIKUYHXYGGJMLM-UUOKFMHZSA-N | 
| Pubchem ID | 65085 | 
| 存储条件 | In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C | 
| 溶解方案 | DMSO: 25 mg/mL(88.26 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的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 
 
 
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