1. PI3K/Akt/mTOR
  2. PI3K

TGR-1202 (Synonyms: RP5264)

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

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

For research use only. We do not sell to patients.
TGR-1202 Chemical Structure

TGR-1202 Chemical Structure

CAS No. : 1532533-67-7

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $138 In-stock
5 mg $110 In-stock
10 mg $190 In-stock
50 mg $650 In-stock
100 mg $990 In-stock
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  • References

Description

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

IC50 & Target

IC50: 22.2 nM (PI3Kδ)[1]

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
NCT Number Sponsor Condition Start Date Phase
NCT03207256 TG Therapeutics, Inc. Chronic Lymphocytic Leukemia|Non Hodgkin Lymphoma June 28, 2017 Phase 2
NCT02742090 TG Therapeutics, Inc. Chronic Lymphocytic Leukemia April 2016 Phase 2
NCT01767766 TG Therapeutics, Inc.|SCRI Development Innovations, LLC Non-Hodgkin's Lymphoma|Chronic Lymphocytic Leukemia|Peripheral T-Cell Lymphoma|Hodgkin's Lymphoma January 2013 Phase 1
NCT03178201 Changchun Deng|TG Therapeutics, Inc.|Columbia University Follicular Lymphoma July 5, 2017 Phase 2
NCT02164006 TG Therapeutics, Inc. Hodgkin's Lymphoma June 2014 Phase 1
NCT02268851 Dana-Farber Cancer Institute|TG Therapeutics, Inc.|The Leukemia and Lymphoma Society Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma|Mantle Cell Lymphoma November 2014 Phase 1
NCT02100852 TG Therapeutics, Inc. Chronic Lymphocytic Leukemia March 2014 Phase 1
NCT02493530 Vanderbilt-Ingram Cancer Center Myelofibrosis|Polycythemia Vera July 2015 Phase 1
NCT02867618 Changchun Deng|Columbia University Hodgkin Disease|Lymphoma, Non-hodgkin October 16, 2016 Phase 1|Phase 2
NCT02656303 TG Therapeutics, Inc. Chronic Lymphocytic Leukemia January 2016 Phase 2
NCT02574663 TG Therapeutics, Inc.|SCRI Development Innovations, LLC Pancreatic Cancer|Colorectal Cancer|Rectal Cancer|Gastric Cancer|Esophageal Cancer|Gastrointestinal Stromal Tumor (GIST) October 2015 Phase 1
NCT02874404 Matthew Lunning, MD|National Cancer Institute (NCI)|University of Nebraska Recurrent Diffuse Large B-Cell Lymphoma|Refractory Diffuse Large B-Cell Lymphoma October 2016 Phase 2
NCT02006485 TG Therapeutics, Inc. Chronic Lymphocytic Leukemia|Non-Hodgkin's Lymphoma December 2013 Phase 1
NCT02793583 TG Therapeutics, Inc. Diffuse Large B-Cell Lymphoma|Follicular Lymphoma|Marginal Zone Lymphoma|Small Lymphocytic Lymphoma June 2016 Phase 2|Phase 3
NCT02535286 TG Therapeutics, Inc.|Abramson Cancer Center of the University of Pennsylvania Chronic Lymphocytic Leukemia September 2015 Phase 1|Phase 2
NCT02612311 TG Therapeutics, Inc. Chronic Lymphocytic Leukemia January 2016 Phase 3
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References
Molecular Weight

571.55

Formula

C₃₁H₂₄F₃N₅O₃

CAS No.

1532533-67-7

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

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.55% ee.: 99.66%

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Product Name:
TGR-1202
Cat. No.:
HY-12279
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