WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 205938
CAS#: 1532533-67-7 (free base)
Description: Umbralisib, also known as TGR1202 and RP5264 , is a highly specific, orally available, PI3K delta inhibitor, targeting the delta isoform with nanomolar potency and several fold selectivity over the alpha, beta, and gamma isoforms of PI3K. Inhibition of PI3K delta signaling with TGR-1202 has demonstrated robust activity in numerous pre-clinical models and primary cells from patients with hematologic malignancies.
MedKoo Cat#: 205938
CAS#: 1532533-67-7 (free base)
Chemical Formula: C31H24F3N5O3
Exact Mass: 571.18312
Molecular Weight: 571.56
Elemental Analysis: C, 65.14; H, 4.23; F, 9.97; N, 12.25; O, 8.40
Umbralisib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).
Synonym: TGR1202; TGR 1202; TGR-1202; RP5264; RP 5264; RP-5264; Umbralisib.
IUPAC/Chemical Name: (S)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-6-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one
InChi Key: IUVCFHHAEHNCFT-INIZCTEOSA-N
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
SMILES Code: O=C1C(C2=CC=CC(F)=C2)=C([C@@H](N3C4=NC=NC(N)=C4C(C5=CC=C(C(F)=C5)OC(C)C)=N3)C)OC6=CC=C(F)C=C16
The following data is based on the product molecular weight 571.56 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Deng C, Lipstein MR, Scotto L, Jirau Serrano XO, Mangone MA, Li S, Vendome J,
Hao Y, Xu X, Deng SX, Realubit RB, Tatonetti NP, Karan C, Lentzsch S, Fruman DA,
Honig B, Landry DW, O'Connor OA. Silencing c-Myc translation as a therapeutic
strategy through targeting PI3K delta and CK1 epsilon in hematological
malignancies. Blood. 2016 Oct 26. pii: blood-2016-08-731240. [Epub ahead of
print] PubMed PMID: 27784673.
2: Locatelli SL, Careddu G, Inghirami G, Castagna L, Sportelli P, Santoro A,
Carlo-Stella C. The novel PI3K-δ inhibitor TGR-1202 enhances Brentuximab
Vedotin-induced Hodgkin lymphoma cell death via mitotic arrest. Leukemia. 2016
Sep 2. doi: 10.1038/leu.2016.224. [Epub ahead of print] PubMed PMID: 27499137.
3: Brown JR. The PI3K pathway: clinical inhibition in chronic lymphocytic
leukemia. Semin Oncol. 2016 Apr;43(2):260-4. doi:
10.1053/j.seminoncol.2016.02.004. Review. PubMed PMID: 27040704.
1532533-67-7 ( TGR-1202 free base)
1532533-75-7 ( TGR-1202 sulfate)