Download Files:
Umbralisib (tosylate)
SKU
HY-12279A-Get quote
Category Reference compound
Tags Cancer, Casein Kinase;PI3K, Cell Cycle/DNA Damage;PI3K/Akt/mTOR;Stem Cell/Wnt
Products Details
Product Description
– Umbralisib (TGR-1202) tosylate 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 tosylate exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib tosylate can be used for haematological malignancies reseach[1][2][3][4].
Web ID
– HY-12279A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C38H32F3N5O6S
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
– 1532533-72-4
Molecular Weight
– 743.75
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(C7=CC=C(C)C=C7)(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
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.