MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 205938 | Name: Umbralisib
Featured New

Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Umbralisib
Umbralisib
CAS#1532533-67-7 (free base)

Theoretical Analysis

MedKoo Cat#: 205938

Name: Umbralisib

CAS#: 1532533-67-7 (free base)

Chemical Formula: C31H24F3N5O3

Exact Mass: 571.1831

Molecular Weight: 571.56

Elemental Analysis: C, 65.14; H, 4.23; F, 9.97; N, 12.25; O, 8.40

Price and Availability

Size Price Availability Quantity
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
1532533-67-7 (free base) 1532533-75-7 (sulfate) 1532533-78-0 (HCl)
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
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Related CAS# 1532533-67-7 ( TGR-1202 free base) 1532533-75-7 ( TGR-1202 sulfate)      

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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.