A PI3K p110δ inhibitor
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

TGR-1202

Item No. 32877

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(1S)-1-[4-amino-3-[3-fluoro-4-(1-methylethoxy)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-1-yl]ethyl]-6-fluoro-3-(3-fluorophenyl)-4H-1-benzopyran-4-one
CAS Number
1532533-67-7
Synonyms
  • RP 5264
  • Umbralisib
Molecular Formula
C31H24F3N5O3
Formula Weight
571.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 1 mg/ml
λmax
232, 291 nm
SMILES
C[C@@H](C1=C(C2=CC(F)=CC=C2)C(C3=CC(F)=CC=C3O1)=O)N4N=C(C5=CC=C(OC(C)C)C(F)=C5)C6=C(N)N=CN=C46
InChi Code
InChI=1S/C31H24F3N5O3/c1-15(2)41-24-9-7-18(12-22(24)34)27-26-30(35)36-14-37-31(26)39(38-27)16(3)29-25(17-5-4-6-19(32)11-17)28(40)21-13-20(33)8-10-23(21)42-29/h4-16H,1-3H3,(H2,35,36,37)/t16-/m0/s1
InChi Key
IUVCFHHAEHNCFT-INIZCTEOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $75

    Add

    25 mg

    $315

    Add

    50 mg

    $479

    Add

    100 mg

    $662

    Add
    Kinase Resource Center
    Discover Products & Resources for Kinase Research
    • Kinase inhibitors, screening libraries, assay kits, & more
    • Tools to study kinase signaling pathways:
      • Growth factor signaling
      • PI3K/Akt/mTOR
      • MAPKs (ERK, p38, & JNK)
      • JAK/STAT signaling
    • Articles, resources, & advice
    EXPLORE NOW
    Product Description

    TGR-1202 is an inhibitor of PI3K p110δ (IC50 = 22 nM).1 It is selective for p110δ over p110α, p110β, and p110γ (IC50s = >10,000, 1,116, and 1,065 nM, respectively).1,2 TGR-1202 induces apoptosis in patient-derived chronic lymphocytic leukemia lymphocytes when used at concentrations ranging from 0.1 to 25.6 µM.3 In vivo, TGR-1202 (150 mg/kg) reduces tumor growth in a MOLT-4 T cell acute lymphoblastic leukemia (T-ALL) mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lampson, B.L., and Brown, J.R. PI3Kδ-selective and PI3Kα/δ-combinatorial inhibitors in clinical development for B-cell non-Hodgkin lymphoma. Expert Opin. Investig. Drugs 26(11), 1267-1279 (2017).

    2. Deng, C., Lipstein, M.R., Scotto, L., et al. Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood 129(1), 88-99 (2017).

    3. Friedman, D.R., Lanasa, M.C., Brander, D.M., et al. Comparison of the PI3K-δ inhibitors TGR1202 and GS-1101 in inducing cytotoxicity and inhibiting phosphorylation of Akt in CLL cells in vitro. Blood 120(21), 3914 (2012).