GSK2636771 | CAS#1372540-25-4 | PI3K inhibitor

GSK2636771
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205844

CAS#: 1372540-25-4 (free base)

Description: GSK2636771 is an orally bioavailable, substituted benzimidazole inhibitor of the class I phosphoinositide 3-kinase (PI3K) beta isoform with potential antineoplastic activity. PI3K beta inhibitor GSK2636771 selectively inhibits PI3K beta kinase activity in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K beta-expressing and/or PTEN-driven tumor cells. Dysregulation of the PI3K/Akt/mTOR pathway is frequently found in solid tumors and results in the promotion of tumor cell growth, survival, and resistance to both chemotherapy and radiotherapy. PI3K beta is the p110-beta catalytic subunit of the class I PI3K. PTEN, a tumor suppressor protein and negative regulator of PI3K activity, is often mutated in a variety of cancer cells.

Chemical Structure

GSK2636771

CAS# 1372540-25-4 (free base)

Instruction

Theoretical Analysis

MedKoo Cat#: 205844
Name: GSK2636771
CAS#: 1372540-25-4 (free base)
Chemical Formula: C22H22F3N3O3
Exact Mass: 433.16
Molecular Weight: 433.420
Elemental Analysis: C, 60.96; H, 5.12; F, 13.15; N, 9.69; O, 11.07

Price and Availability

Size	Price	Availability
25mg	USD 150	Ready to ship
50mg	USD 250	Ready to ship
100mg	USD 450	Ready to ship
200mg	USD 750	Ready to ship
500mg	USD 1450	Ready to ship
1g	USD 2250	Ready to ship
2g	USD 3650	Ready to ship
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 #: 1372540-25-4 (free base) 2108806-07-9 (HCl) 1372540-91-4 (tris)

Synonym: GSK2636771; GSK-2636771; GSK 2636771

IUPAC/Chemical Name: 2-methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid.

InChi Key: XTKLTGBKIDQGQL-UHFFFAOYSA-N

InChi Code: InChI=1S/C22H22F3N3O3/c1-13-15(4-3-5-18(13)22(23,24)25)12-28-14(2)26-20-17(21(29)30)10-16(11-19(20)28)27-6-8-31-9-7-27/h3-5,10-11H,6-9,12H2,1-2H3,(H,29,30)

SMILES Code: O=C(C1=C2C(N(CC3=CC=CC(C(F)(F)F)=C3C)C(C)=N2)=CC(N4CCOCC4)=C1)O

Appearance: white 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:

Certificate of Analysis:

View CoA: current batch, Lot#KB20828

QC Data:

View QC data: current batch, Lot#KB20828

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

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 433.42 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: Weigelt B, Warne PH, Lambros MB, Reis-Filho JS, Downward J. PI3K pathway dependencies in endometrioid endometrial cancer cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3533-44. doi: 10.1158/1078-0432.CCR-12-3815. Epub 2013 May 14. PubMed PMID: 23674493; PubMed Central PMCID: PMC3700760.

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