Umbralisib

CAS No. 1532533-67-7

Umbralisib ( RP 5264;TGR1202;TGR-1202 )

Catalog No. M12154 CAS No. 1532533-67-7

Umbralisib (RP5264,TGR1202, TGR-1202) 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
2MG 53 In Stock
5MG 87 In Stock
10MG 160 In Stock
25MG 324 In Stock
50MG 426 In Stock
100MG 624 In Stock
200MG Get Quote In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    Umbralisib
  • Note
    Research use only, not for human use.
  • Brief Description
    Umbralisib (RP5264,TGR1202, TGR-1202) is a potent, selective, orally available PI3Kδ inhibitor with IC50 of 22 nM.
  • Description
    Umbralisib (RP5264,TGR1202, TGR-1202) 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 1 uM.Blood Cancer Phase 3 Clinical
  • Synonyms
    RP 5264;TGR1202;TGR-1202
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    PI3K
  • Recptor
    PI3Kδ
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1532533-67-7
  • Formula Weight
    571.55
  • Molecular Formula
    C31H24F3N5O3
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    O=C1C(C2=CC=CC(F)=C2)=C([C@@H](N3N=C(C4=CC=C(OC(C)C)C(F)=C4)C5=C(N)N=CN=C53)C)OC6=CC=C(F)C=C16
  • Chemical Name
    4H-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)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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.
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