WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406323
CAS#: 900185-02-6
Description: PIK-294 is a highly selective inihibitor 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.
MedKoo Cat#: 406323
Name: PIK-294
CAS#: 900185-02-6
Chemical Formula: C28H23N7O2
Exact Mass: 489.19
Molecular Weight: 489.52792
Elemental Analysis: C, 68.70; H, 4.74; N, 20.03; O, 6.54
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
The following data is based on the product molecular weight 489.52792 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 |
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.
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