Umbralisib tosylate
Based on 5 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 1532533-72-4
- Formula: C38H32F3N5O6S
- Molecular Weight:743.75
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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 tosylate
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Biological Activity
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PI3Kδ 6.2 nM (Kd) |
PI3Kγ 1400 nM (Kd) |
PI3Kβ >10000 nM (Kd) |
PI3Kα >10000 nM (Kd) |
Umbralisib tosylate causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[3].
Umbralisib tosylate (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner in human lymphoma and leukemia cell lines[4].
Umbralisib tosylate (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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1532533-72-4
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Molecular Weight 743.75
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Formula C38H32F3N5O6S
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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(C7=CC=C(C)C=C7)(O)=O
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Synonyms
TGR-1202 tosylate; RP5264 tosylate
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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 tosylate Related Classifications
HY-12279A Related Classifications
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