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  3. Umbralisib hydrochloride

Umbralisib hydrochloride (Synonyms: TGR-1202 hydrochloride; RP5264 hydrochloride)

Cat. No.: HY-12279C Purity: 99.63%
Handling Instructions

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

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

Umbralisib hydrochloride Chemical Structure

Umbralisib hydrochloride Chemical Structure

CAS No. : 1532533-78-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 161 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 220 In-stock
Estimated Time of Arrival: December 31
25 mg USD 440 In-stock
Estimated Time of Arrival: December 31
50 mg USD 580 In-stock
Estimated Time of Arrival: December 31
100 mg USD 990 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Umbralisib hydrochloride (TGR-1202 hydrochloride) is a novel PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively; Umbralisib hydrochloride (TGR-1202 hydrochloride) 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 (TGR-1202; 10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. Umbralisib and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and carfilzomib 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 (TGR-1202; 150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2].

Clinical Trial
Molecular Weight

608.01

Formula

C₃₁H₂₅ClF₃N₅O₃

CAS No.

1532533-78-0

SMILES

#116Ybr5kUkt8bhz8Nkz8NktCi9z8bhpZUktvN+x8Jmn3J4bYyr53JkNZU+5ZUkt YNkt8ag53UktCi9z8b8p8bUz8am/3U4z8N4z8bUb3UkpYNk7ZU+5ZUktCig5ZUkA +i0MXsr5Mx==

Shipping

Room temperature in continental US; may vary elsewhere.

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 : ≥ 150 mg/mL (246.71 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6447 mL 8.2235 mL 16.4471 mL
5 mM 0.3289 mL 1.6447 mL 3.2894 mL
10 mM 0.1645 mL 0.8224 mL 1.6447 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.11 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

UmbralisibTGR-1202RP5264TGR1202TGR 1202RP 5264RP-5264PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Product name:
Umbralisib hydrochloride
Cat. No.:
HY-12279C
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