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

Umbralisib  (Synonyms: TGR-1202; RP5264)

Cat. No.: HY-12279 Purity: 98.69%
COA Handling Instructions

Umbralisib (TGR-1202) 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 exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib can be used for haematological malignancies reseach.

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

Umbralisib Chemical Structure

Umbralisib Chemical Structure

CAS No. : 1532533-67-7

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Solution
10 mM * 1 mL in DMSO USD 151 In-stock
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10 mM * 1 mL
ready for reconstitution
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Solid
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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

Other Forms of Umbralisib:

Umbralisib Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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CK1 CK2

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Umbralisib (TGR-1202) 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 exhibits unique immunomodulatory effects on chronic lymphocytic leukemia (CLL) T cells. Umbralisib 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 causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[3].
? Umbralisib (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner in human lymphoma and leukemia cell lines[4].
? 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[4].

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

Umbralisib Related Antibodies
In Vivo

Umbralisib (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

571.55

Appearance

Solid

Formula

C31H24F3N5O3
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
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 : 25 mg/mL (43.74 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 available by MCE.
Purity & Documentation

Purity: 98.69%

COA (254 KB) LCMS (270 KB)

Handling Instructions (2659 KB)
References
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Umbralisib 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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  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Umbralisib1532533-67-7TGR-1202 RP5264TGR1202TGR 1202RP5264RP 5264RP-5264PI3KCasein KinasePhosphoinositide 3-kinaseCLL T cellshaematological malignanciescancerlymphocytic leukemialymphomaorally activeInhibitorinhibitorinhibit

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