PIK-75


Catalog No. Size PriceQuantity
M11405-2 2mg solid $90
M11405-10 10mg solid $270

Description

PIK-75 was developed as part of a PI 3-kinase drug discovery program. PIK75 attenuates insulin stimulation of Akt/PKB in a range of cell types at 100 nM. The compound has been reported to block growth of a range of cell lines with an IC50 value in the region of 50 nM. In vivo studies have shown that PIK-75, administered at 50 mg/kg, inhibited the growth of HeLa cell xenografts in mice models.

Product information

CAS Number: 372196-67-3

Molecular Weight: 452.28

Formula: C16H14BrN5O4S

Synonym:

PIK 75

Related CAS Number:

372196-77-5 (HCl)

Chemical Name: (E)-N'-((6-bromoimidazo[1, 2-a]pyridin-3-yl)methylene)-N, 2-dimethyl-5-nitrobenzenesulfonohydrazide

Smiles: CN(/N=C/C1=CN=C2C=CC(Br)=CN12)S(=O)(=O)C1=CC(=CC=C1C)[N+]([O-])=O

InChiKey: QTHCAAFKVUWAFI-DJKKODMXSA-N

InChi: InChI=1S/C16H14BrN5O4S/c1-11-3-5-13(22(23)24)7-15(11)27(25,26)20(2)19-9-14-8-18-16-6-4-12(17)10-21(14)16/h3-10H,1-2H3/b19-9+

Technical Data

Appearance: Solid Power

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

Solubility: DMSO: 4 mg/mLwarmed(8.18 mM).

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:

PIK-75 shows the impressive potency and isoform selectivity at p110α while the corresponding IC50 values are 1300 nM, 76 nM and 510 nM for other PI3K isoforms, p110β, -γ, and -δ, respectively. Furthermore, when binding to purified p110α, PIK-75 is a noncompetitive inhibitor with respect to ATP with Ki of 36 nM and competitive with respect to the substrate PI with Ki of 2.3 nM. PIK-75 also shows potent inhibition of DNA-PK. PIK-75 (1 μM) reduces cell survival by significantly decreasing mitochondrial activity in unstimulated nonasthmatic airway smooth muscle (ASM) cells, asthmatic ASM cells, and lung fibroblasts. While in TGFβ-stimulated ASM cells, PIK75 only decreases mitochondrial activity in asthmatic cells without effects in nonasthmatic cells. A recent study shows that PIK-75 (10 nM) inhibits TNF-α-induced CD38 mRNA expression and significantly attenuates of TNF-α-induced ADP-ribosyl cyclase activity in human airway smooth muscle cells.

In Vivo:

In the ErbB3WT tumor model, PIK-75 reduces in vitro chemotactic response to HRGβ1 and lowers pAkt levels by 40%. Besides, PIK-75 significantly reduces tumor cell motility and in vivo invasion in ErbB3WT primary tumors. In the CD1 male mice, PIK-75 leads to serious impairments in the insulin tolerance test (ITT) and glucose tolerance test (GTT), and an increase in glucose production during a pyruvate tolerance test (PTT).

References:

  1. Moir LM, et al. J Pharmacol Exp Ther. 2011, 337(2), 557-566.
  2. WO/2003/072557, 09/04/2003
  3. Zheng Z, et al. Mol Pharmacol. 2011, 80(4), 657-664.

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

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