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Product Description
– Umbralisib (TGR-1202) sulfate is an orally active, potent and selective dual PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor, with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib sulfate can be used for haematological malignancies reseach[1][2][3][4].
Web ID
– HY-12279B
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C31H26F3N5O7S
References
– [1]Maharaj K, et al. The dual PI3Kδ/CK1ε inhibitor umbralisib exhibits unique immunomodulatory effects on CLL T cells. Blood Adv. 2020 Jul 14;4(13):3072-3084.|[2]Burris HA 3rd, et al. Umbralisib, a novel PI3Kδ and casein kinase-1ε inhibitor, in relapsed or refractory chronic lymphocytic leukaemia and lymphoma: an open-label, phase 1, dose-escalation, first-in-human study. Lancet Oncol. 2018 Apr;19(4):486-496.|[3]Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth.|[4]Deng C, et al. Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood. 2017 Jan 5;129(1):88-99.
CAS Number
– 1532533-75-7
Molecular Weight
– 669.63
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.O=S(O)(O)=O
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Casein Kinase;PI3K
Isoform
– CK1;PI3Kα;PI3Kβ;PI3Kγ;PI3Kδ
Pathway
– Cell Cycle/DNA Damage;PI3K/Akt/mTOR;Stem Cell/Wnt
Product type
– Reference compound
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