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I-BET151
CAS No. 1300031-49-5
I-BET151 ( GSK1210151A;I-BET 151;GSK-1210151A )
Catalog No. M11204 CAS No. 1300031-49-5
I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 53 | In Stock |
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| 5MG | 87 | In Stock |
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| 10MG | 105 | In Stock |
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| 25MG | 192 | In Stock |
|
| 50MG | 321 | In Stock |
|
| 100MG | 480 | In Stock |
|
| 500MG | 1071 | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameI-BET151
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NoteResearch use only, not for human use.
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Brief DescriptionI-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor.
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DescriptionI-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL; demonstrates potent efficacy against cell lines harbouring different MLL-fusions (MOLM13 cell IC50=120 nM, MV4:11 cell IC50=26 nM), induices early cell cycle arrest and apoptosis, selectively abrogates BRD3/4 recruitment to chromatin;shows significant therapeutic value and survival benefit in mouse models of murine MLL-AF9 and human MLL-AF4 leukaemia.
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SynonymsGSK1210151A;I-BET 151;GSK-1210151A
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PathwayChromatin/Epigenetic
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TargetBromodomain
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RecptorBRD2;BRD3;BRD4
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number1300031-49-5
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Formula Weight415.44
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Molecular FormulaC23H21N5O3
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESO=C(N1[C@@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3
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Chemical Name2H-Imidazo[4,5-c]quinolin-2-one, 7-(3,5-dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-
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. Dawson MA, et al. Nature. 2011 Oct 2;478(7370):529-33.
2. Mirguet O, et al. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7.
3. Chaidos A, et al. Blood. 2014 Jan 30;123(5):697-705.
4. Wyspiańska BS, et al. Leukemia. 2014 Jan;28(1):88-97.
2. Mirguet O, et al. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7.
3. Chaidos A, et al. Blood. 2014 Jan 30;123(5):697-705.
4. Wyspiańska BS, et al. Leukemia. 2014 Jan;28(1):88-97.
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