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

Size Price Stock Quantity
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
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Other Forms of TGR-1202:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • 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
View MoreCollapse
References
Preparing Stock Solutions
Concentration Volume 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

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%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

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