CC-885是一种新型的cereblon (CRBN)调节剂,其通过招募GSPT1蛋白至CRL4(CRBN) E3泛素连接酶复合物,促进GSPT1的泛素化和降解。CC-885具有在多种癌症研究中具有潜在的应用价值,特别是那些依赖于特定蛋白质稳定性的肿瘤类型。


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| 产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
95% | |||||||||||||||||
| Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
| Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
| PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
| MRT68921 HCl |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
| ROC-325 | ✔ | 99%+ | |||||||||||||||||
| Autophinib |
+++
Autophagy, IC50: 40 nM |
99% | |||||||||||||||||
| Lys05 | ✔ | 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。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | CC-885是一种新型的cereblon (CRBN)调节剂,其通过招募GSPT1蛋白至CRL4(CRBN) E3泛素连接酶复合物,促进GSPT1的泛素化和降解。CC-885具有在多种癌症研究中具有潜在的应用价值,特别是那些依赖于特定蛋白质稳定性的肿瘤类型。 |
| 体内研究 | CC-885在293FT人胚胎肾细胞以及AML细胞系NB-4、MOLM-13和OCI-AML2中具有抑制细胞增殖的作用(IC50<0.01μM)。此外,为评价CC-885对人MM细胞系RPMI8226和MM1S细胞的抗增殖作用,采用不同浓度(6.25~50 nM) CC-885处理MM细胞系1 ~ 3天。CCk8实验显示,CC-885对MM细胞产生剂量依赖性和时间依赖性的生长抑制作用。 |
| 体外研究 | CC-885是一种新型的cereblon (CRBN)调节剂,其通过招募GSPT1蛋白至CRL4(CRBN) E3泛素连接酶复合物,促进GSPT1的泛素化和降解。CC-885具有在多种癌症研究中具有潜在的应用价值,特别是那些依赖于特定蛋白质稳定性的肿瘤类型。 |
| Concentration | Treated Time | Description | References | |
| HeLa cells | 1 μM | 24 h | To assess the effect of CC-885 on BNIP3L-mediated mitophagy. | Acta Pharmacol Sin. 2020 Sep;41(9):1246-1254 |
| HEK293T cells | 1 μM | 24 h | To verify whether CC-885-induced BNIP3L protein degradation is CRBN-dependent. | Acta Pharmacol Sin. 2020 Sep;41(9):1246-1254 |
| A549 cells | 200 nM | 12 h | To identify potential neosubstrates of CC-885 in A549 cells using quantitative proteomics analysis. | Acta Pharmacol Sin. 2020 Sep;41(9):1246-1254 |
| NCI-H1299 cells | 50 nM | 24 h | This synergistic effect was also obtained in another NSCLC cell line, NCI-H1299. | Mol Ther Oncolytics. 2020 Jun 23;18:215-225 |
| A549 cells | 50 nM | 24 h | CC-885 synergistically enhanced volasertib-induced cell death in NSCLC identified by IMiD drug screen. | Mol Ther Oncolytics. 2020 Jun 23;18:215-225 |
| U87 glioblastoma cells | 100 nM | 16 h | To confirm the ubiquitination effect of CC-885 on GSPT1 via the E3 ubiquitin ligase complex (CRL4CBRN) | Cell Death Dis. 2024 Aug 8;15(8):572 |
| LX2 cells | 1 μM | 24 h | To evaluate the inhibitory effect of CC-885 on BNC2 expression, results showed CC-885 significantly reduced BNC2 protein levels | Nat Commun. 2022 Sep 10;13(1):5324 |
| HDQ-P1 cells | 10 nM | 72 h | CC-885 efficiently reduced eRF3a levels starting a few h after compound addition and reaching >90% reduction within 24h. | Nucleic Acids Res. 2021 Apr 19;49(7):3692-3708 |
| Administration | Dosage | Frequency | Description | References | ||
| BALB/cA nude mice | A549 xenograft model | Intraperitoneal injection | 20 mg/kg | Three times per week for four weeks | While volasertib and CC-885 alone inhibited tumor growth, the combination of both small molecular drugs markedly inhibited tumor growth and reduced tumor weights. | Mol Ther Oncolytics. 2020 Jun 23;18:215-225 |
| Nude mice | U87 glioblastoma cell transplanted brain tumor model | Intraperitoneal injection | 50 mg/kg and 100 mg/kg | Once every alternate day, total of 4 times | To assess the therapeutic effect of CC-885 on transplanted brain tumors, showing significantly prolonged survival and reduced tumor size | Cell Death Dis. 2024 Aug 8;15(8):572 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.27mL 0.45mL 0.23mL |
11.34mL 2.27mL 1.13mL |
22.68mL 4.54mL 2.27mL |
|
| CAS号 | 1010100-07-8 |
| 分子式 | C22H21ClN4O4 |
| 分子量 | 440.88 |
| SMILES Code | O=C(NCC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2)=O)C=C1)NC4=CC=C(C)C(Cl)=C4 |
| MDL No. | MFCD31657329 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | DOEVCIHTTTYVCC-UHFFFAOYSA-N |
| Pubchem ID | 24788636 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,Store in freezer, under -20°C |
| 溶解方案 |
DMSO: 65 mg/mL(147.43 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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