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PIK-75 (hydrochloride)

CAT: 0804-HY-13281-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-13281-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) [1][2]. PIK-75 hydrochloride induces apoptosis[3].
CAS Number
372196-77-5
UNSPSC
12352005
Hazard Statement
H302
Target
Apoptosis; DNA-PK; PI3K
Type
Reference compound
Related Pathways
Apoptosis; Cell Cycle/DNA Damage; PI3K/Akt/mTOR
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/pik-75.html
Purity
99.66
Solubility
DMSO : 11 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
BrC(C=C1)=CN2C1=NC=C2/C=N/N(S(=O)(C3=C(C=CC([N+]([O-])=O)=C3)C)=O)C.[H]Cl
Molecular Formula
C16H15BrClN5O4S
Molecular Weight
488.74
Precautions
H302
References & Citations
[1]Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125 (4) :733-47.|[2]Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404 (3) :449-58.|[3]Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44 (3) :959-69.|[4]Hayakawa M, Kawaguchi K, Kaizawa H, et al. Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007;15 (17) :5837-5844.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PI3KC2α; PI3KC2β; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ; Vps34
Citation 01
Clin Cancer Res. 2020 Apr 15;26 (8) :2011-2021. |Res Sq. 2023 Apr 6:rs.3.rs-2688694.|Adv Sci (Weinh) . 2024 Jun 3:e2400023.|Cell Rep. 2025 Feb 5;44 (2) :115246.|Molecules. 2020 Apr 23;25 (8) :1980.

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