MedKoo Biosciences

Umbralisib
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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.

Chemical Structure

Umbralisib

CAS# 1532533-67-7 (free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 205938
Name: Umbralisib
CAS#: 1532533-67-7 (free base)
Chemical Formula: C31H24F3N5O3
Exact Mass: 571.18
Molecular Weight: 571.560
Elemental Analysis: C, 65.14; H, 4.23; F, 9.97; N, 12.25; O, 8.40

Price and Availability

Size	Price	Availability
25mg	USD 450	2 Weeks
50mg	USD 750	2 Weeks
100mg	USD 1250	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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)

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

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.

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

Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

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Umbralisib featured