Umbralisib

Umbralisib (TGR-1202) 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 exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach[1][2][3][4].

Product Specifications

CAS Number

[1532533-67-7]

Product Name Alternative

TGR-1202; RP5264

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Casein Kinase; PI3K

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/TGR-1202.html

Concentration

10mM

Purity

98.94

Solubility

DMSO : 25 mg/mL (ultrasonic)

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

Molecular Formula

C31H24F3N5O3

Molecular Weight

571.55

Precautions

H302, H315, H319, H335

References & Citations

[1]Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth.|[2]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|[3]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.|[4]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.