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CB-5083
CAS No. 1542705-92-9
CB-5083 ( CB5083 | CB 5083 )
产品货号. M12188 CAS No. 1542705-92-9
CB-5083 是一种有效的、选择性的、口服生物可利用的 p97 AAA 抑制剂，IC50 为 11 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 2MG | ￥437 | 有现货 |
|
| 5MG | ￥721 | 有现货 |
|
| 10MG | ￥1126 | 有现货 |
|
| 25MG | ￥2535 | 有现货 |
|
| 50MG | ￥3993 | 有现货 |
|
| 100MG | ￥5856 | 有现货 |
|
| 500MG | ￥12312 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称CB-5083
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述CB-5083 是一种有效的、选择性的、口服生物可利用的 p97 AAA 抑制剂，IC50 为 11 nM。
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产品描述CB-5083 is a potent, selective, orally bioavailable inhibitor of p97 AAA with IC50 of 11 nM, specifically targets D2 ATPase site of p97, shows 9.6, 128 and 158-fold less affinity for DNA-PK, mTOR and PIK3C3; causes accumulation of poly-ubiquitinated proteins, retention of ERAD substrates, and generation of irresolvable proteotoxic stress, leading to activation of the apoptotic arm of the unfolded protein response (UPR) in cancer cells; inhibits A549 cell viability with IC50 of 0.67 uM, induces the UPR and apoptosis in xenograft tumor models.Blood Cancer Phase 1 Clinical.
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体外实验——
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体内实验Animal Model:Nu/Nu nude female mice bearing established human tumor xenografts derived from HCT 116 colon Dosage:75 mg/kg Administration:Administered orally using every day (qd) dosing, for 2 weeks. Result:Showed more profound antitumor activity.
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同义词CB5083 | CB 5083
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通路Proteasome/Ubiquitin
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靶点p97
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受体p97
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研究领域Cancer
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适应症Blood cancer
化学信息
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CAS Number1542705-92-9
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分子量413.4717
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分子式C24H23N5O2
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纯度>98% (HPLC)
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溶解度10 mM in DMSO
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SMILESO=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N.
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化学全称1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Anderson DJ, et al. Cancer Cell. 2015 Nov 9;28(5):653-665.
2. Zhou HJ, et al. J Med Chem. 2015 Dec 24;58(24):9480-97.
3. Le Moigne R, et al. Mol Cancer Ther. 2017 Nov;16(11):2375-2386.
4. Bastola P, et al. Mol Oncol. 2016 Dec;10(10):1559-1574.
