PI3K-IN-2


Catalog No. Size PriceQuantity
M24631-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

PI3K-IN-2 (compound 10) is a potent and orally active PI3Kβ/δ (IC50=7.1/8.6 nM) inhibitor with excellent selectivity versus PI3Kσ and PI3Kγ (IC50=13/190 nM, respectively).

Product information

CAS Number: 1403458-28-5

Molecular Weight: 525.54

Formula: C28H29F2N3O5

Chemical Name: 8-[(2R)-1-(3,5-difluorophenyl)pyrrolidin-2-yl]-2-(morpholin-4-yl)-6-(morpholine-4-carbonyl)-4H-chromen-4-one

Smiles: O=C(C1=CC([C@H]2CCCN2C2C=C(F)C=C(F)C=2)=C2OC(=CC(=O)C2=C1)N1CCOCC1)N1CCOCC1

InChiKey: CPFXYHKMOTWOFK-XMMPIXPASA-N

InChi: InChI=1S/C28H29F2N3O5/c29-19-14-20(30)16-21(15-19)33-3-1-2-24(33)22-12-18(28(35)32-6-10-37-11-7-32)13-23-25(34)17-26(38-27(22)23)31-4-8-36-9-5-31/h12-17,24H,1-11H2/t24-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

PI3K-IN-2 (compound 10) shows PI3Kβ cell IC50 1.1 nM in phosphatase and tensin homolog (PTEN) null MDA-MB-468 cell and PI3Kδ cell IC50 14 nM in Jeko-1 B-cell.

In Vivo:

PI3K-IN-2 shows profound pharmacodynamic modulation of AKT phosphorylation in PTEN-deficient PC3 prostate tumour bearing mice after oral administration and gave significant inhibition of tumour growth in the same xenograft model.

Products are for research use only. Not for human use.

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