Umbralisib sulfate
Based on 5 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 1532533-75-7
- Formula: C31H26F3N5O7S
- Molecular Weight:669.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Umbralisib sulfate
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Biological Activity
Description
IC50 & Target
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PI3Kδ 6.2 (Kd) |
PI3Kγ 1400 (Kd) |
PI3Kα >10000 (Kd) |
PI3Kβ >10000 (Kd) |
In Vitro
Umbralisib sulfate causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[3].
In human lymphoma and leukemia cell lines, Umbralisib sulfate (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner[4].
Umbralisib sulfate (15-50 μM) potently represses the expression of c-Myc in the DLBCL cell line LY7, and is uniquely characterized with structural features suitable for targeting CK1ε in lymphoma cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1532533-75-7
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Molecular Weight 669.63
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Formula C31H26F3N5O7S
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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
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Synonyms
TGR-1202 sulfate; RP-5264 sulfate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Evolutionary states and trajectories characterized by distinct pathways stratify patients with ovarian high grade serous carcinoma. [Abstract]2023 Jun 12;41(6):1103-1117.e12. PMID: 37207655 -
Phytomedicine
CBX5 loss drives Pl3Kδ inhibitor resistance in mantle cell lymphoma and propolis restores sensitivity by inducing CBX5-mediated ferroptosis. [Abstract]2025 Jul 25:143:156911. PMID: 40466505 -
NPJ Precis Oncol
Integrative profiling strategies to guide personalized therapy in mantle cell lymphoma: a pilot study. [Abstract]2025 Nov 21;9(1):373. PMID: 41272086 -
J Med Chem
Discovery of ( S)-2-(1-(4-Amino-3-(3-fluoro-4-methoxyphenyl)-1 H-pyrazolo[3,4- d]pyrimidin-1-yl)propyl)-3-cyclopropyl-5-fluoroquinazolin-4(3 H)-one (IHMT-PI3Kδ-372) as a Potent and Selective PI3Kδ Inhibitor for the Treatment of Chronic Obstructive Pulmonary Disease. [Abstract]2020 Nov 25;63(22):13973-13993. PMID: 33180507 -
Mol Pharm
2022 Nov 7;19(11):4320-4332. PMID: 36269563
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Umbralisib sulfate Related Classifications
HY-12279B Related Classifications
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