1. PI3K/Akt/mTOR Stem Cell/Wnt Cell Cycle/DNA Damage
  2. PI3K Casein Kinase
  3. Umbralisib hydrochloride

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

Cat. No.: HY-12279C Purity: 98.98%
COA Handling Instructions

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.

Umbralisib hydrochloride Chemical Structure

Umbralisib hydrochloride Chemical Structure

CAS No. : 1532533-78-0

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 161 In-stock
Solution
10 mM * 1 mL in DMSO USD 161 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 220 In-stock
25 mg USD 440 In-stock
50 mg USD 580 In-stock
100 mg USD 990 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

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  • Biological Activity

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  • References

  • Customer Review

Description

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[1][2][3][4].

IC50 & Target[1]

PI3Kδ

22.2 nM (EC50)

PI3Kδ

6.2 nM (Kd)

PI3Kγ

1400 nM (Kd)

PI3Kβ

>10000 nM (Kd)

PI3Kα

>10000 nM (Kd)

In Vitro

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.

In Vivo

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

608.01

Appearance

Solid

Formula

C31H25ClF3N5O3

CAS No.
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

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)

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 available by MedChemExpress (MCE).
Purity & Documentation
References
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Umbralisib hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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