1. PI3K/Akt/mTOR
  2. PI3K

Umbralisib (Synonyms: TGR-1202; RP5264)

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

TGR-1202 is a PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively.

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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Customer Review

Other Forms of Umbralisib:

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

TGR-1202 is a PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively.

IC50 & Target[1]

PI3Kδ

22.2 nM (IC50)

In Vitro

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, TGR-1202 (10 nM-100 μM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. TGR-1202 and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. TGR-1202 and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. TGR-1202 (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, TGR-1202 (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

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.
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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