2. PI3K/Akt/mTOR
  3. PI3K Akt mTOR
  4. KTC1101

KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response.

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KTC1101 Chemical Structure

KTC1101 Chemical Structure

CAS No. : 2764833-47-6

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Customer Review

Based on 1 publication(s) in Google Scholar

KTC1101 Related Antibodies

Top Publications Citing Use of Products

View All PI3K Isoform Specific Products:

View All Isoforms
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All mTOR Isoform Specific Products:

View All Isoforms
mTOR mTORC1 mTORC2

  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

KTC1101 is an orally active pan-PI3K inhibitor. KTC1101 can inhibit the PI3K signaling pathway, reduce downstream AKT and mTOR phosphorylation, and reduces the expression of Ki67. The anti-tumor effect of KTC1101 has a dual mechanism of action: directly inhibiting tumor cell growth and dynamically enhancing immune response[1].

IC50 & Target

Ki67

 

PI3Kα

3.72 nM (IC50)

PI3Kβ

36.29 nM (IC50)

PI3Kδ

1.22 nM (IC50)

PI3Kγ

17.09 nM (IC50)

PI3K

 

In Vitro

KTC1101 (0.1-50000 nM, 48 h) can dose-dependently induce cell cycle stagnation in G1 phase in all tested cell lines (PC3, TMD8, HSC2, HSC4, and CAL33 cells). KTC1101 has anti-proliferative activity, with the IC50 ranging from 20 nM to 130 nM, but has no significant promotion of apoptosis[1].
KTC1101 (0.1-1000 nM, 1 h) exhibits significant inhibitory activity against all PI3K isoforms in the Adapta kinase assay. The IC50 values of KTC1101 for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ are 3.72 nM, 36.29 nM, 1.22 nM and 17.09 nM respectively[1].
KTC1101 (0-125 nM, 48 h) effectively inhibits the PI3K signaling pathway in WB experiments, reduces the phosphorylation of PI3K downstream effectors AKT and mTOR[1].

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

KTC1101 Related Antibodies

Cell Viability Assay[1]

Cell Line: 39 human tumor cell lines, PC3, TMD8, HSC2, HSC4, CAL33 cells, etc.
Concentration: 0.1, 1, 10, 100, 1000, 25000, 50000 nM
Incubation Time: 48 h
Result: Exhibited an average GI50 value of 23.4 nM across all cell lines tested, significantly lower than ZSTK474 (HY-50847) (320 nM) and Copanlisib (HY-15346) (134 nM).

Western Blot Analysis[1]

Cell Line: PC3 cells, TMD8 cells
Concentration: 0, 5, 25, 125 nM
Incubation Time: 48 h
Result: Showed better inhibitory performance in TMD8 cells compared with ZSTK474 (HY-50847) and Copanlisib (HY-15346).
In Vivo

KTC1101 (0-125 mg/kg/day for 14 days, p.o.) can arrest tumor growth in mice with human tumor xenografts and show no signs of recurrence[1].

Pharmacokinetic Analysis in tumor xenograft mouse model[1]

Route Dose (mg/kg) t1/2 (h) Tmax (h) Cmax (μg/mL) AUC0-t (μg/mL*h) Vz/F> (L/kg) CLz/F (L/h/kg)
p.o. 100 7.19 0.67 1.66 9.33 117.96 10.71

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

476.48

Formula

C21H26F2N8O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)C1=NC2=C(OC)C=C(N)C=C2N1C3=NC(N4CCOCCC4)=NC(N5CCOCC5)=N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (69.95 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 2.0987 mL 10.4936 mL 20.9872 mL
5 mM 0.4197 mL 2.0987 mL 4.1974 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

×
Volume (start)

V1

=
Concentration (final)

C2

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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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (10.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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
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 2.0987 mL 10.4936 mL 20.9872 mL 52.4681 mL
5 mM 0.4197 mL 2.0987 mL 4.1974 mL 10.4936 mL
10 mM 0.2099 mL 1.0494 mL 2.0987 mL 5.2468 mL
15 mM 0.1399 mL 0.6996 mL 1.3991 mL 3.4979 mL
20 mM 0.1049 mL 0.5247 mL 1.0494 mL 2.6234 mL
25 mM 0.0839 mL 0.4197 mL 0.8395 mL 2.0987 mL
30 mM 0.0700 mL 0.3498 mL 0.6996 mL 1.7489 mL
40 mM 0.0525 mL 0.2623 mL 0.5247 mL 1.3117 mL
50 mM 0.0420 mL 0.2099 mL 0.4197 mL 1.0494 mL
60 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8745 mL
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KTC1101 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:

KTC11012764833-47-6KTC 1101KTC-1101PI3KAktmTORPhosphoinositide 3-kinasePKBProtein kinase BMammalian target of RapamycinTumor microenvironmentCD8+ T cellsImmunotherapy synergyCell cycleCell proliferationInhibitorinhibitorinhibit

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