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活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
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C408056-1ml |
1ml |
现货 ![]() |
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英文别名 | 1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl- |
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规格或纯度 | 10mM in DMSO |
英文名称 | CB-5083 |
生化机理 | CB-5083 是一种强效、选择性、可口服的 p97 AAA ATPase 抑制剂,IC50 为 11 nM。第一阶段 |
储存温度 | -80℃储存 |
运输条件 | 超低温冰袋运输 |
产品介绍 |
CB-5083是一种有效的,选择性的,且口服具有生物活性的p97 AAA ATPase抑制剂,IC50为 11 nM。Phase 1。 Information CB-5083 CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1. In A549 cells, CB-5083 causes significant K48 poly-ubiquitinated protein and CHOP accumulation as well as p62 reduction, and kills tumor cells with IC50 of 680 nM. In vivo In mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) also results in significant tumor growth inhibition. cell lines: Concentrations:~40.0 μM Incubation Time:72 h Powder Purity:≥98% |
ALogP | 3.748 |
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hba_count | 4 |
HBD Count | 2 |
Rotatable Bond | 5 |
分子类型 | 小分子 |
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Canonical SMILES | CC1=CC2=C(C=CC=C2C(N)=O)[N]1C3=NC4=C(COCC4)C(=N3)NCC5=CC=CC=C5 |
分子量 | 413.47 |
Reaxy-Rn | 26539278 |
Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26539278&ln= |
DMSO(mg / mL) Max Solubility | 82 |
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DMSO(mM) Max Solubility | 198.32 |
Water(mg / mL) Max Solubility | <1 |
Reaxy-Rn | 26539278 |
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Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26539278&ln= |
Record the entire process by video | Conform |
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Concentration(Compounding value) | 9-11(mmol/L) |