Art. -Nr.: HY-13281

PIK-75 hydrochloride

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

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). PIK-75 hydrochloride induces apoptosis.

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Reinheit: 99.66%
CAS. Nr.: 372196-77-5
Formel: C₁₆H₁₅BrClN₅O₄S
Molecular Weight:488.74

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

PIK-75 hydrochloride Chemical Structure

CAS. Nr.: 372196-77-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

DNA-PK

2 nM (IC₅₀)

p110α

5.8 nM (IC₅₀)

p110γ

76 nM (IC₅₀)

p110δ

510 nM (IC₅₀)

p110β

1.3 μM (IC₅₀)

hsVPS34

2.6 μM (IC₅₀)

PI3KC2β

1 μM (IC₅₀)

PI3KC2α

10 μM (IC₅₀)

mTORC1

1 μM (IC₅₀)

mTORC2

10 μM (IC₅₀)

ATM

2.3 μM (IC₅₀)

ATR

21 μM (IC₅₀)

PI4KIIIβ

50 μM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A-375	IC₅₀	0.058 μM Compound: 8c	Inhibition of serum-induced proliferation of human A375 cells Inhibition of serum-induced proliferation of human A375 cells	[PMID: 17601739]
A549	IC₅₀	0.069 μM Compound: 8c	Inhibition of serum-induced proliferation of human A549 cells Inhibition of serum-induced proliferation of human A549 cells	[PMID: 17601739]
HeLa	IC₅₀	0.051 μM Compound: 8c	Inhibition of serum-induced proliferation of human HeLa cells Inhibition of serum-induced proliferation of human HeLa cells	[PMID: 17601739]
MCF7	IC₅₀	0.019 μM Compound: 8c	Inhibition of serum-induced proliferation of human MCF7 cells Inhibition of serum-induced proliferation of human MCF7 cells	[PMID: 17601739]
MCF7	IC₅₀	0.039 μM Compound: 8c	Inhibition of serum-induced proliferation of human adriamycin-resistant MCF7 cells Inhibition of serum-induced proliferation of human adriamycin-resistant MCF7 cells	[PMID: 17601739]
Sf9	IC₅₀	0.04 μM Compound: 8c	Inhibition of His-tagged human p110gamma expressed in SF9/Baculovirus system by SPA Inhibition of His-tagged human p110gamma expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	0.1 μM Compound: 8c	Inhibition of glu-tagged PI3K C2-beta expressed in SF9/Baculovirus system by SPA Inhibition of glu-tagged PI3K C2-beta expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	0.85 μM Compound: 8c	Inhibition of GST-tagged human p110-beta expressed in SF9/Baculovirus system by SPA Inhibition of GST-tagged human p110-beta expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	0.0003 μM Compound: 8c	Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]
Sf9	IC₅₀	0.3 nM Compound: 8c	Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA	[PMID: 17601739]

In Vitro

PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC₅₀s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively^[1].
PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC₅₀ values of 1.2 and 1.3 μM, respectively^[1].
PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC₅₀ of 78 nM^[2].
PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death^[3].
PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[3]

Cell Line:

Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1)
Concentration:

0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM
Incubation Time:

48 hours
Result:

Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment.

Western Blot Analysis^[2]

Cell Line:

Overnight-starved CHO-IR cells
Concentration:

1, 10, 100, 1000 nM
Incubation Time:

5 minutes
Result:

Blocked the phosphorylation of PKB induced by insulin (1 nM, 10 min) on both Ser473and Thr308 in a dose-dependent manner.

In Vivo

PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Mice bearing tumors of MIA PaCa-2^[3]
Dosage:

2 mg/kg; or combination with Gemcitabine (20 mg/kg)
Administration:

Administered injection; 5 times per week. 25 days
Result:

Reduced the tumor growth and enhanced the antitumor effect.

Chemical Information

CAS. Nr. 372196-77-5
Appearance Solid
Molecular Weight 488.74
Formel C₁₆H₁₅BrClN₅O₄S
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (5)

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Journal Impact Factor

Adv Sci (Weinh)

TRIM24 Cooperates with Ras Mutation to Drive Glioma Progression through snoRNA Recruitment of PHAX and DNA-PKcs. [Abstract]

2024 Jun 3:e2400023. PMID: 38828688
Clin Cancer Res

Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]

2020 Apr 15;26(8):2011-2021. PMID: 31937620
Cell Rep

Meteorin-like alleviates hepatic steatosis by regulating hepatic triglyceride secretion and fatty acid oxidation. [Abstract]

2025 Feb 5;44(2):115246. PMID: 39918960
Molecules

In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei. [Abstract]

2020 Apr 23;25(8):1980. PMID: 32340370
Res Sq

Haploinsufficiency of ZNF251 causes DNA-PKcs-dependent resistance to PARP inhibitors in BRCA1-mutated cancer cells. [Abstract]

2023 Apr 6:rs.3.rs-2688694. PMID: 37066268

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 11 mg/mL (22.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0461 mL

10.2304 mL

20.4608 mL

5 mM

0.4092 mL

2.0461 mL

4.0922 mL

10 mM

0.2046 mL

1.0230 mL

2.0461 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.1 mg/mL (2.25 mM); Clear solution

This protocol yields a clear solution of ≥ 1.1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.1 mg/mL (2.25 mM); Clear solution

This protocol yields a clear solution of ≥ 1.1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.1 mg/mL (2.25 mM); Clear solution

This protocol yields a clear solution of ≥ 1.1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (11.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0461 mL	10.2304 mL	20.4608 mL	51.1519 mL
	5 mM	0.4092 mL	2.0461 mL	4.0922 mL	10.2304 mL
	10 mM	0.2046 mL	1.0230 mL	2.0461 mL	5.1152 mL
	15 mM	0.1364 mL	0.6820 mL	1.3641 mL	3.4101 mL
	20 mM	0.1023 mL	0.5115 mL	1.0230 mL	2.5576 mL

Keywords

PIK-75 hydrochloride

5 Cited Publications

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PIK-75 hydrochloride

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Publications Citing Use of MedChemExpress (MCE) PIK-75 hydrochloride

Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PIK-75 hydrochloride Related Classifications

HY-13281 Related Classifications