Cat. No.: HY-162382

KTC1101

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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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Pureté: 98.09%
CAS No.: 2764833-47-6
Formule: C₂₁H₂₆F₂N₈O₃
Masse moléculaire:476.48

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

KTC1101 Chemical Structure

CAS No.: 2764833-47-6

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

Ki67

PI3Kα

3.72 nM (IC₅₀)

PI3Kβ

36.29 nM (IC₅₀)

PI3Kδ

1.22 nM (IC₅₀)

PI3Kγ

17.09 nM (IC₅₀)

PI3K

Voir tous les produits spécifiques à Isoform PI3K :

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform mTOR :

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.

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)	t_1/2 (h)	T_max (h)	C_max (μg/mL)	AUC_0-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.

Chemical Information

CAS No. 2764833-47-6
Appearance Solid
Masse moléculaire 476.48
Formule C₂₁H₂₆F₂N₈O₃
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

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

2.0987 mL

10.4936 mL

20.9872 mL

5 mM

0.4197 mL

2.0987 mL

4.1974 mL

10 mM

0.2099 mL

1.0494 mL

2.0987 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 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 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instruction de manipulation (2659 KB)

Références

[1]. Peng X, et al. A novel pan-PI3K inhibitor KTC1101 synergizes with anti-PD-1 therapy by targeting tumor suppression and immune activation. Mol Cancer. 2024 Mar 14;23(1):54. [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

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

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Bioactive Compound Library Max

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Bioactive Compound Library

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Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

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Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

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Posttranslational Modification Library

Lactylation Compound Library

Voir tous les produits spécifiques à Isoform PI3K

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform mTOR

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

KTC1101 Related Classifications

HY-162382 Related Classifications