Umbralisib
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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.


Chemical Structure

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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: 571.18312
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
100.0mg USD 2350.0 2 Weeks
200.0mg USD 2950.0 2 Weeks
500.0mg USD 3650.0 2 Weeks
1.0g USD 4950.0 2 Weeks
2.0g USD 8650.0 2 Weeks
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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

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

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 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.

Umbralisib

100.0mg / USD 2350.0


Additional Information

Related CAS#
1532533-67-7 ( TGR-1202 free base)
1532533-75-7 ( TGR-1202 sulfate)