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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > DNA Damage & DNA Repai > CC-115CAS：1228013-15-7
Molecular Formula：C16H16N8O
Molecular Weight：336.35
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Solid
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| CAS | 1228013-15-7 |
| Name | CC-115 |
| Molecular Formula | C16H16N8O |
| Molecular Weight | 336.35 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD29036965 |
| SMILES | O=C1CN=C2C(N1CC)=NC(C3=C(C)N=C(C4=NN=CN4)C=C3)=CN2 |
| Target Point | DNA-PK，mTOR，PI3Kα |
| Passage | DNA Damage/DNA Repair |
| Background | Compound 401 is a DNA-PK and mTOR inhibitor |
| Biological Activity | CC-115是DNA依赖性的蛋白激酶DNA-PK和哺乳动物雷帕霉素靶标mTOR的双重抑制剂，IC50分别为0.013 μM 和 0.021 μM。具有潜在的抗肿瘤活性。[1-2] |
| In Vitro | CC-115在CLL细胞中抑制DNA损伤修复途径和TORK，并在休眠CLL细胞中引起caspase引来的细胞死亡。其诱导细胞死亡的IC50为0.51 μM。CC-115能够恢复CD40诱导产生的化学抗性，在CLL细胞中减少在CD40的刺激下诱导的Mcl-1，Bfl-1和Bcl-XL的表达。它还能抑制CLL细胞的增殖。在健康的B细胞中，CC-115诱导细胞死亡，IC50为0.93 μM。CC-115 and NU7441能够完全阻滞CD4+和CD8+ T细胞的增殖。总的来说，CC-115能够诱导直接毒性作用，抑制对于CLL生存、化学抗性、增殖十分重要的信号通路[1]。 |
| In Vivo | 在慢性淋巴细胞性白血病患者(CLL患者)中，CC-115减少其淋巴结病[1]。在多种物种中，CC-115具有良好的体内药代动力学分布，在小鼠、大鼠、狗中的口服生物利用度分别为53%、76%、~100%。CC-115具有有利的物理化学和药代动力学性质，在体内可抑制mTOR信号通路并抑制肿瘤生长。在体内体外实验中都具有药物安全性，适合于临床药物开发[2]。 |
| Cell Experiment | 用不同浓度的CC-115(0.35，1，3.5 μM)处理新鲜分离的CLL细胞30分钟。然后，将细胞暴露于5-Gy γ辐射中或用10 μg/mL bleomycin处理，30分钟。收集细胞裂解液。[1] |
| Data Literature Source | [1] Thijssen R，et al. Blood. 2016，128(4):574-83. [2] Mortensen DS，et al. J Med Chem. 2015，58(14):5599-608. |
| Unit | Bottle |
| Specification | 2mg 5mg |
Compound 401是DNA-PK和mTOR抑制剂
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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