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TGR-1202 hydrochloride
CAS No. 1532533-78-0
TGR-1202 hydrochloride ( RP5264 hydrochloride;TGR1202 hydrochloride;TGR 1202 hydrochloride )
Catalog No. M12156 CAS No. 1532533-78-0
TGR-1202 (RP5264,TGR1202,Umbralisib) is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 50MG | 568 | Get Quote |
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| 100MG | Get Quote | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameTGR-1202 hydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionTGR-1202 (RP5264,TGR1202,Umbralisib) is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM.
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DescriptionTGR-1202 (RP5264,TGR1202,Umbralisib) is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM, 50-fold selectivity over PI3Kα/β and >10,000 fold over PI3Kγ; enhances Brentuximab Vedotin-induced Hodgkin lymphoma cell death via mitotic arrest, demonstrates highly synergistic effect with the proteasome inhibitor carfilzomib in lymphoma, leukemia, and myeloma cell lines and primary lymphoma and leukemia cells; synergistically disrupts the 4E-BP1-eIF4F-c-Myc axis with carfilzomib, also potently inhibits 60% of the activity of CK1ε at 1uM.Blood Cancer Phase 3 Clinical
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SynonymsRP5264 hydrochloride;TGR1202 hydrochloride;TGR 1202 hydrochloride
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PathwayPI3K/Akt/mTOR signaling
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TargetPI3K
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RecptorPI3K
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number1532533-78-0
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Formula Weight608.01
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Molecular FormulaC31H25ClF3N5O3
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Purity>98% (HPLC)
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SolubilityDMSO
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SMILESCC(C)OC1=C(C=C(C=C1)C2=NN(C3=NC=NC(=C23)N)C(C)C4=C(C(=O)C5=C(O4)C=CC(=C5)F)C6=CC(=CC=C6)F)F.Cl
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Chemical Name4H-1-Benzopyran-4-one, 2-[(1S)-1-[4-amino-3-[3-fluoro-4-(1-methylethoxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)-, hydrochloride (1:1)
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. Locatelli SL, et al. Leukemia. 2016 Dec;30(12):2402-2405.
2. Deng C, et al. Blood. 2017 Jan 5;129(1):88-99.
3. Burris HA 3rd, et al. Lancet Oncol. 2018 Feb 20. pii: S1470-2045(18)30082-2.
4. Lampson BL, et al. Expert Opin Investig Drugs. 2017 Nov;26(11):1267-1279.
2. Deng C, et al. Blood. 2017 Jan 5;129(1):88-99.
3. Burris HA 3rd, et al. Lancet Oncol. 2018 Feb 20. pii: S1470-2045(18)30082-2.
4. Lampson BL, et al. Expert Opin Investig Drugs. 2017 Nov;26(11):1267-1279.
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