PIK-294 | CAS#900185-02-6 | PI3K inhibitor

MedKoo Cat#: 406323 | Name: PIK-294

Description:

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

PIK-294 is a highly selective inhibitor of the phosphoinositide 3-kinase (PI3K) p110δ with an IC50 value of 10 nM compared to IC50 values of 10 μM, 490 nM and 160 nM for PI3Kα/β/γ, respectively. PIK-294 has been used to help distinguish the unique roles of the various PI3-K isoforms. PIK-294 inhibited both chemokinetic and chemotactic CXCL8-induced migration.

Chemical Structure

PIK-294

CAS#900185-02-6

Theoretical Analysis

MedKoo Cat#: 406323

Name: PIK-294

CAS#: 900185-02-6

Chemical Formula: C28H23N7O2

Exact Mass: 489.1913

Molecular Weight: 489.53

Elemental Analysis: C, 68.70; H, 4.74; N, 20.03; O, 6.54

Price and Availability

Size	Price	Availability
10mg	USD 150.00	2 Weeks
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 800.00	2 Weeks

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Related CAS #

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Synonym

PIK294; PIK 294; PIK-294.

IUPAC/Chemical Name

2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-(o-tolyl)quinazolin-4(3H)-one

InChi Key

WFSLJOPRIJSOJR-UHFFFAOYSA-N

InChi Code

InChI=1S/C28H23N7O2/c1-16-7-3-4-12-21(16)35-22(32-20-11-5-8-17(2)23(20)28(35)37)14-34-27-24(26(29)30-15-31-27)25(33-34)18-9-6-10-19(36)13-18/h3-13,15,36H,14H2,1-2H3,(H2,29,30,31)

SMILES Code

O=C1N(C2=CC=CC=C2C)C(CN3N=C(C4=CC=CC(O)=C4)C5=C(N)N=CN=C53)=NC6=C1C(C)=CC=C6

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

Information about this agent

Product Data

Product Data

Instruction

View handling instruction

Biological target:

PIK-294 is a potent p110δ-selective inhibitor with an IC50 of 10 nM.

In vitro activity:

Analysis of the specific Class I PI3 Kinase catalytic isoforms alpha, delta and gamma using the inhibitors PIK-75, PIK-294 and AS-605240 respectively indicated differential roles in CXCL8-induced neutrophil migration. PIK-294 inhibited both chemokinetic and chemotactic CXCL8-induced migration. Reference: PLoS One. 2015 Feb 6;10(2):e0116250. https://pubmed.ncbi.nlm.nih.gov/25659107/

In vivo activity:

TBD

	Solvent	mg/mL	mM
Solubility
	Ethanol	0.3	0.51

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 489.53 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:

Martin KJ, Muessel MJ, Pullar CE, Willars GB, Wardlaw AJ. The role of phosphoinositide 3-kinases in neutrophil migration in 3D collagen gels. PLoS One. 2015 Feb 6;10(2):e0116250. doi: 10.1371/journal.pone.0116250. Erratum in: PLoS One. 2015;10(7):e0134924. PMID: 25659107; PMCID: PMC4320071.

In vitro protocol:

In vivo protocol:

TBD

1. Inhibitors of the PI3k/Akt/Ikk/NF-kb signalling pathway, pharmaceutically acceptable salts thereof and compositions containing said inhibitors for prophylaxis and treatment of viral diseases. Fedichev, Petr Olegovich; Vinnik, Andrey Alexandrovich. PCT Int. Appl. (2013), WO 2013147649 A2 20131003 . 2. Methods for predicting cancer treatment responsiveness to phosphatidylinositol 3-kinase (PI3K) inhibitors. Jane, Stephen M.; Darido, Charbel. PCT Int. Appl. (2013), WO 2013029116 A1 20130307. 3. Methods for treating oncovirus positive cancers. Jimeno, Antonio; Hausman, Diana F.; Peterson, Scott. PCT Int. Appl. (2012), WO 2012118978 A1 20120907. 4. Use of phosphatidylinositol-3'-kinase (PI3K) p110 delta isoform inhibitors for treating retroviral infection and replication. Katsikis, Peter D.; Boesteanu, Alina C.; Turner, Martin. PCT Int. Appl. (2012), WO 2012009452 A1 20120119. 5. Methods and compositions for treatment of ophthalmic conditions. Wilson, Troy Edward; Rommel, Christian; Liu, Yi; Ren, Pingda. PCT Int. Appl. (2010), WO 2010059593 A1 20100527. 6. Discovery of Dual Inhibitors of the Immune Cell PI3Ks p110δ and p110γ: A Prototype for New Anti-inflammatory Drugs. Williams, Olusegun; Houseman, Benjamin T.; Kunkel, Eric J.; Aizenstein, Brian; Hoffman, Randy; Knight, Zachary A.; Shokat, Kevan M. Chemistry & Biology (Cambridge, MA, United States) (2010), 17(2), 123-134. 7. Preparation of pyrazolopyrimidinylmethyl quinazolinones as PI3 kinase antagonists. Knight, Zachary A.; Shokat, Kevan M.; Williams, Olesegun. PCT Int. Appl. (2008), WO 2008127226 A2 20081023. 8.Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Apsel, Beth; Blair, Jimmy A.; Gonzalez, Beatriz; Nazif, Tamim M.; Feldman, Morri E.; Aizenstein, Brian; Hoffman, Randy; Williams, Roger L.; Shokat, Kevan M.; Knight, Zachary A. Nature Chemical Biology (2008), 4(11), 691-699. 9.A pharmacological map of the PI3-K family defines a role for p110α in insulin signaling. Knight, Zachary A.; Gonzalez, Beatriz; Feldman, Morri E.; Zunder, Eli R.; Goldenberg, David D.; Williams, Olusegun; Loewith, Robbie; Stokoe, David; Balla, Andras; Toth, Balazs; et al. Cell (Cambridge, MA, United States) (2006), 125(4), 733-747.