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  3. Umbralisib

Umbralisib (Synonyms: TGR-1202; RP5264)

Cat. No.: HY-12279 Purity: 98.55% ee.: 99.66%
Handling Instructions

Umbralisib (TGR-1202) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib (TGR-1202) is also active against CK1ε, with an EC50 value of 6.0 μM.

For research use only. We do not sell to patients.

Umbralisib Chemical Structure

Umbralisib Chemical Structure

CAS No. : 1532533-67-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 166 In-stock
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Estimated Time of Arrival: December 31
10 mg USD 228 In-stock
Estimated Time of Arrival: December 31
50 mg USD 780 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1188 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

Umbralisib (TGR-1202) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib (TGR-1202) is also active against CK1ε, with an EC50 value of 6.0 μM.

IC50 & Target

PI3Kδ

22.2 nM (IC50)

In Vitro

Umbralisib (RP5264) causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[1]. In human lymphoma and leukemia cell lines, Umbralisib (RP5264; 10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. Umbralisib and PR-171 synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and PR-171 in combination synergistically and selectively silence the c-Myc and E2F transcription programs. Umbralisib (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[2].

In Vivo

In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, Umbralisib (RP5264; 150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2].

Clinical Trial
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (34.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7496 mL 8.7481 mL 17.4963 mL
5 mM 0.3499 mL 1.7496 mL 3.4993 mL
10 mM 0.1750 mL 0.8748 mL 1.7496 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (3.50 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Molecular Weight

571.55

Formula

C₃₁H₂₄F₃N₅O₃

CAS No.

1532533-67-7

SMILES

O=C1C(C2=CC=CC(F)=C2)=C([[email protected]@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

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 98.55% ee.: 99.66%

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Product Name:
Umbralisib
Cat. No.:
HY-12279
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Umbralisib

Cat. No.: HY-12279