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Umbralisib

CAT: 0804-HY-12279-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-12279-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
CK1; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ

Alternative Products

CatalogName
205938Umbralisib
T17066Umbralisib hydrochloride
MBS5814888Umbralisib sulfate
MBS5814848Umbralisib tosylate
MBS5754038Umbralisib R-enantiomer
C13255-01Umbralisib (TGR-1202)
MBS3841541-01TGR-1202 (Umbralisib)

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