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CB-5083
CAS No. 1542705-92-9
CB-5083( CB5083 | CB 5083 )
Catalog No. M12188 CAS No. 1542705-92-9
CB-5083 is a potent, selective, orally bioavailable inhibitor of p97 AAA with IC50 of 11 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 49 | In Stock |
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| 5MG | 80 | In Stock |
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| 10MG | 125 | In Stock |
|
| 25MG | 282 | In Stock |
|
| 50MG | 444 | In Stock |
|
| 100MG | 651 | In Stock |
|
| 500MG | 1368 | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameCB-5083
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NoteResearch use only, not for human use.
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Brief DescriptionCB-5083 is a potent, selective, orally bioavailable inhibitor of p97 AAA with IC50 of 11 nM.
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DescriptionCB-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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In Vitro——
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In VivoAnimal 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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SynonymsCB5083 | CB 5083
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PathwayProteasome/Ubiquitin
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Targetp97
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Recptorp97
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number1542705-92-9
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Formula Weight413.4717
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Molecular FormulaC24H23N5O2
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Purity>98% (HPLC)
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Solubility10 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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Chemical Name1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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.
molnova catalog
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