2. Cell Cycle/DNA Damage Epigenetics PI3K/Akt/mTOR Apoptosis
  3. PARP PI3K Apoptosis
  4. PARP/PI3K-IN-1

PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases.

For research use only. We do not sell to patients.

PARP/PI3K-IN-1 Chemical Structure

PARP/PI3K-IN-1 Chemical Structure

CAS No. : 2337386-47-5

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Customer Review

Based on 1 publication(s) in Google Scholar

PARP/PI3K-IN-1 Related Antibodies

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PARP/PI3K-IN-1 (compound 15) is a potent PARP/PI3K inhibitor with pIC50 values of 8.22, 8.44, 8.25, 6.54, 8.13, 6.08 for PARP-1, PARP-2, PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively. PARP/PI3K-IN-1 is a highly effective anticancer compound targeted against a wide range of oncologic diseases[1].

IC50 & Target[1]

PARP-1

8.22 (pIC50)

PARP-2

8.44 (pIC50)

PI3Kα

8.25 (pIC50)

PI3Kβ

6.54 (pIC50)

PI3Kδ

8.13 (pIC50)

PI3Kγ

6.08 (pIC50)

In Vitro

PARP/PI3K-IN-1 (compound 15; 1 μM; 72 hours) leads to a significant increase in cell apoptosis[1].
PARP/PI3K-IN-1 (1 μM; 72 hours) reduces the autophosphorylation levels of AKT and S6 while increases the autophosphorylation level of ERK after treating cells, indicating that it can inhibit the PI3K pathway and activate the ERK pathway[1].
PARP/PI3K-IN-1 (1 μM) displays a strong capability to downregulate the expression of BRCA1/2 at the mRNA level in MDA-MB-468 cancer cells[1].
PARP/PI3K-IN-1 not only shows significant inhibitory activity against BRCA-deficient cells HCC1937 and HCT116, but also displays potent anti-proliferative activity against BRCA-proficient cells MDA-MB-231 and MDA-MB-468[1].

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

PARP/PI3K-IN-1 Related Antibodies

Apoptosis Analysis[1]

Cell Line: MDA-MB-468 cancer cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Led to a significant increase in cell apoptosis.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cancer cells
Concentration: 1 μM
Incubation Time: 72 hours
Result: Reduced the autophosphorylation levels of AKT and S6 while increased the autophosphorylation level of ERK after treating cells.
In Vivo

PARP/PI3K-IN-1 (i.p.; 50 mg/kg; twice daily (BID) for 34 consecutive days) significantly suppresses the tumor growth[1].

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

Animal Model: Six-week-old male BALB/c nude mice with MDA-MB-468 cells[1]
Dosage: 50 mg/kg
Administration: i.p.; twice daily (BID) for 34 consecutive days
Result: Significantly suppressed the tumor growth.
Molecular Weight

660.62

Formula

C33H28F4N8O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NN=C(CC2=CC=C(F)C(C(N3CCC4=C(N5CCOCC5)N=C(C6=C(C(F)(F)F)C=C(N)N=C6)N=C4C3)=O)=C2)C7=C1C=CC=C7
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (151.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5137 mL 7.5686 mL 15.1373 mL
5 mM 0.3027 mL 1.5137 mL 3.0275 mL
View the Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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: ≥ 2.5 mg/mL (3.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (3.78 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.43%

SDS (251 KB)

COA (249 KB) HNMR (161 KB) RP-HPLC (160 KB) LCMS (115 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5137 mL 7.5686 mL 15.1373 mL 37.8432 mL
5 mM 0.3027 mL 1.5137 mL 3.0275 mL 7.5686 mL
10 mM 0.1514 mL 0.7569 mL 1.5137 mL 3.7843 mL
15 mM 0.1009 mL 0.5046 mL 1.0092 mL 2.5229 mL
20 mM 0.0757 mL 0.3784 mL 0.7569 mL 1.8922 mL
25 mM 0.0605 mL 0.3027 mL 0.6055 mL 1.5137 mL
30 mM 0.0505 mL 0.2523 mL 0.5046 mL 1.2614 mL
40 mM 0.0378 mL 0.1892 mL 0.3784 mL 0.9461 mL
50 mM 0.0303 mL 0.1514 mL 0.3027 mL 0.7569 mL
60 mM 0.0252 mL 0.1261 mL 0.2523 mL 0.6307 mL
80 mM 0.0189 mL 0.0946 mL 0.1892 mL 0.4730 mL
100 mM 0.0151 mL 0.0757 mL 0.1514 mL 0.3784 mL
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PARP/PI3K-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PARP/PI3K-IN-12337386-47-5PARPPI3KApoptosispoly ADP ribose polymerase Phosphoinositide 3-kinaseAnticanceroncologicanti-proliferativeBRCA1-deficientbreastcancercolorectaltriple-negativeInhibitorinhibitorinhibit

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