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Umbralisib sulfate (TGR-1202; RP-5264) is a novel and potent PI3Kδ and casein kinase-1-ε (CK1ε) inhibitor. It is orally bioactive, potently and selectively inhibits dual targets PI3Kδ and casein kinase-1-ε (CK1ε) with EC50 of 22.2 nM and 6.0 μM, respectively. Umbralisib sulfate shows immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells and can be used for haematological malignancies.
| ln Vitro |
Umbralisib sulfate inhibits human whole blood CD19 cell proliferation to half its half-maximum at concentrations between 100 and 300 nM [3]. Umbralisib sulfate (10 nM–100 μM) suppresses Ser473 phosphorylated AKT in concentration-dependent manner in human lymphoma and leukemia cell lines [4]. With its distinct structural characteristics, umbralisib sulfate (15–50 μM) can efficiently suppress the expression of c-Myc in the DLBCL cell line LY7 and can also target CK1ε in lymphoma cells [4].
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| ln Vivo |
Using the MOLT-4 cell line in a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL), umbralisib sulfate (150 mg/kg, po daily) dramatically decreased the size of the tumor at day 25 tumors[4].
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| 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.
[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. [3]. Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth. [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. |
| Molecular Formula |
C31H26F3N5O7S
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|---|---|
| Molecular Weight |
669.627656459808
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| CAS # |
1532533-75-7
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| Related CAS # |
Umbralisib;1532533-67-7;Umbralisib hydrochloride;1532533-78-0;Umbralisib tosylate;1532533-72-4
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| SMILES |
S(=O)(=O)(O)O.FC1C=CC2=C(C=1)C(C(C1C=CC=C(C=1)F)=C([C@H](C)N1C3C(=C(N)N=CN=3)C(C3C=CC(=C(C=3)F)OC(C)C)=N1)O2)=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4934 mL | 7.4668 mL | 14.9336 mL | |
| 5 mM | 0.2987 mL | 1.4934 mL | 2.9867 mL | |
| 10 mM | 0.1493 mL | 0.7467 mL | 1.4934 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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