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TGR-1202

Cat. No. M5268
TGR-1202 Structure
Size Price Availability Quantity
5mg USD 130 In stock
10mg USD 210 In stock
50mg USD 550 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: The compound displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, the compound causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 results initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrate that the compound causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells.

In vivo: The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.

Protocol
Cell Experiment
Cell lines Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells
Preparation method Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells are incubated with desired concentrations of RP5264. Growth is assessed after 96 h by a MTT assay.
Concentrations
Incubation time 96 h
Animal Experiment
Animal models Female Balb/c mice
Formulation
Dosages 12.5, 25, 50 mg/kg
Administration 12.5, 25, 50 mg/kg
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 571.55
Formula C31H24F3N5O3
CAS Number 1532533-67-7
Purity >99%
Solubility 100 mg/mL in DMSO
Storage at -20°C
References

Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies.
Deng C, et al. Blood. 2017 Jan 5;129(1):88-99. PMID: 27784673.

The novel PI3K-δ inhibitor TGR-1202 enhances Brentuximab Vedotin-induced Hodgkin lymphoma cell death via mitotic arrest.
Locatelli SL, et al. Leukemia. 2016 Dec;30(12):2402-2405. PMID: 27499137.

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Keywords: TGR-1202 supplier, PI3K, inhibitors

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