Umbralisib hydrochloride
Based on 5 publication(s) in Google Scholar
Umbralisib (TGR-1202) hydrochloride 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 hydrochloride exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib hydrochloride can be used for haematological malignancies reseach.
For research use only. We do not sell to patients.
- Purity: 99.04%
- CAS No.: 1532533-78-0
- Formula: C31H25ClF3N5O3
- Molecular Weight:608.01
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Kinase Inhibitor Library
HY-L009
-
PI3K/Akt/mTOR Compound Library
HY-L015
-
Stem Cell Signaling Compound Library
HY-L017
-
Wnt/Hedgehog/Notch Compound Library
HY-L020
-
FDA-Approved Drug Library
HY-L022
-
Anti-Cancer Compound Library
HY-L025
-
Autophagy Compound Library
HY-L029
-
Anti-Aging Compound Library
HY-L034
-
Drug Repurposing Compound Library
HY-L035
-
Differentiation Inducing Compound Library
HY-L038
-
Oxygen Sensing Compound Library
HY-L045
-
Glycolysis Compound Library
HY-L058
-
Cytoskeleton Compound Library
HY-L060
-
Orally Active Compound Library
HY-L061
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
Anti-Cancer Metabolism Compound Library
HY-L083
-
Anti-Obesity Compound Library
HY-L087
-
Angiogenesis-Related Compound Library
HY-L088
-
Glucose Metabolism Compound Library
HY-L092
-
Anti-Liver Cancer Compound Library
HY-L101
-
Rare Diseases Drug Library
HY-L102
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
FDA-Approved Anticancer Drug Library
HY-L122
-
Human Metabolite Library
HY-L123
-
Anti-Prostate Cancer Compound Library
HY-L124
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Cancer Stem Cells Compound Library
HY-L135
-
Heterocyclic Compound Library
HY-L138
-
Pain-Related Compound Library
HY-L139
-
Membrane Protein-targeted Compound Library
HY-L149
-
Highly Selective Inhibitors Library
HY-L158
-
Serine/Threonine Kinase Inhibitor Library
HY-L164
-
Anti-Hematopathy Compound Library
HY-L171
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Anti-Fibrosis Compound Library
HY-L185
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Rheumatic Arthritis Compound Library
HY-L210
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Posttranslational Modification Library
HY-L226
-
FDA Kinase Inhibitor Library
HY-L230
-
Lactylation Compound Library
HY-L249
Publications Citing Use of MedChemExpress (MCE) Umbralisib hydrochloride
More
Biological Activity
|
PI3Kδ 22.2 nM (EC50) |
PI3Kδ 6.2 nM (Kd) |
PI3Kγ 1400 nM (Kd) |
PI3Kβ >10000 nM (Kd) |
PI3Kα >10000 nM (Kd) |
Umbralisib hydrochloride causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[3].
Umbralisib hydrochloride (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner in human lymphoma and leukemia cell lines[4].
Umbralisib hydrochloride (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.
Chemical Information
-
CAS No. 1532533-78-0
-
Appearance Solid
-
Molecular Weight 608.01
-
Formula C31H25ClF3N5O3
-
Color White to off-white
-
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.[H]Cl
-
Synonyms
TGR-1202 hydrochloride; RP5264 hydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
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
Solvent & Solubility
DMSO : ≥ 150 mg/mL (246.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6447 mL | 8.2235 mL | 16.4471 mL | 41.1177 mL |
| 5 mM | 0.3289 mL | 1.6447 mL | 3.2894 mL | 8.2235 mL | |
| 10 mM | 0.1645 mL | 0.8224 mL | 1.6447 mL | 4.1118 mL | |
| 15 mM | 0.1096 mL | 0.5482 mL | 1.0965 mL | 2.7412 mL | |
| 20 mM | 0.0822 mL | 0.4112 mL | 0.8224 mL | 2.0559 mL | |
| 25 mM | 0.0658 mL | 0.3289 mL | 0.6579 mL | 1.6447 mL | |
| 30 mM | 0.0548 mL | 0.2741 mL | 0.5482 mL | 1.3706 mL | |
| 40 mM | 0.0411 mL | 0.2056 mL | 0.4112 mL | 1.0279 mL | |
| 50 mM | 0.0329 mL | 0.1645 mL | 0.3289 mL | 0.8224 mL | |
| 60 mM | 0.0274 mL | 0.1371 mL | 0.2741 mL | 0.6853 mL | |
| 80 mM | 0.0206 mL | 0.1028 mL | 0.2056 mL | 0.5140 mL | |
| 100 mM | 0.0164 mL | 0.0822 mL | 0.1645 mL | 0.4112 mL |
Umbralisib hydrochloride Related Classifications
HY-12279C Related Classifications
Powered by Bioz