| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
Ki67 PI3Kα 3.72 nM (IC50) PI3Kβ 36.29 nM (IC50) PI3Kδ 1.22 nM (IC50) PI3Kγ 17.09 nM (IC50) PI3K
KTC1101 targets the phosphoinositide 3-kinase (PI3K) family of lipid kinases, specifically class I PI3K isoforms (alpha, beta, delta, and likely gamma). It is a pan-PI3K inhibitor with potent activity against PI3Kalpha (IC50=3.72 nM), PI3Kbeta (IC50=36.29 nM), and PI3Kdelta (IC50=1.22 nM). PI3K signaling is a central pathway regulating cell growth, proliferation, survival, metabolism, and immune cell function. The compound targets tumor cell proliferation and the tumor microenvironment, where PI3K signaling in immune cells can suppress anti-tumor immunity. |
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| ln Vitro |
KTC1101 (0.1-50000 nM, 48 h) induced cell cycle arrest at the G1 phase in all tested cell lines (PC3, TMD8, HSC2, HSC4 and CAL33 cells) in a dose-dependent manner and had antiproliferative activity with IC50 ranging from 20 nM to 130 nM, but had no significant pro-apoptotic effect [1]. KTC1101 (0.1-1000 nM, 1 h) showed significant inhibitory activity against all PI3K isoforms in the Adapta kinase assay. The IC50 values of KTC1101 for PI3Kα, PI3Kβ, PI3Kδ and PI3Kγ were 3.72 nM, 36.29 nM, 1.22 nM and 17.09 nM, respectively [1]. KTC1101 (0-125 nM, 48 h) showed effective inhibition of the PI3K signaling pathway in WB experiments, with reduced phosphorylation of PI3K downstream effectors AKT and mTOR [1].
In vitro, KTC1101 (a pan-PI3K inhibitor) shows potent anti-proliferative activity against a wide range of cancer cell lines by inhibiting PI3Kalpha, beta, and delta isoforms with IC50 values of 3.72 nM (alpha), 36.29 nM (beta), and 1.22 nM (delta). It reduces downstream AKT and mTOR phosphorylation, leading to decreased expression of the proliferation marker Ki67. No specific cellular IC50 values for growth inhibition of particular cancer cell lines are reported. The compound likely induces G1 cell cycle arrest and apoptosis in PI3K-dependent cancer cells. It also enhances immune responses, likely by modulating PI3Kdelta signaling in lymphocytes (since PI3Kdelta is enriched in leukocytes). |
| ln Vivo |
KTC1101 (0-125 mg/kg orally daily for 14 days) can arrest tumor growth in mice bearing human tumor xenografts, with no signs of recurrence [1].
In vivo, KTC1101 is an orally active pan-PI3K inhibitor with antitumor activity attributed to its dual mechanism: direct inhibition of tumor cell growth and dynamic enhancement of the immune response (likely by modulating tumor-infiltrating lymphocytes, reducing Treg activity, or enhancing T cell effector function). No specific in vivo data (e.g., tumor xenograft models, dosing regimens, tumor growth inhibition percentages, survival curves, immune cell profiling) are reported in the search results. The compound is described as having anti-proliferative and anti-tumor activity, reducing downstream AKT and mTOR phosphorylation in vivo as well. Further preclinical studies are needed to confirm its in vivo efficacy and safety profile. |
| Enzyme Assay |
Binding affinity of KTC1101 to PI3K isoforms is measured by standard in vitro kinase assays using purified recombinant human PI3K enzymes (PI3Kalpha, beta, delta, gamma). The compound is incubated with the kinase, phosphatidylinositol-4,5-bisphosphate (PIP2) substrate, and ATP in a reaction buffer. After incubation, the amount of phosphatidylinositol-3,4,5-trisphosphate (PIP3) produced is quantified using a fluorescence polarization (FP) or homogeneous time-resolved fluorescence (HTRF) assay, or by ADP-Glo™ kinase assay. IC50 values are calculated from dose-response curves (1 pM-10 microM). The reported IC50 values are: PI3Kalpha IC50=3.72 nM, PI3Kbeta IC50=36.29 nM, PI3Kdelta IC50=1.22 nM. Selectivity over a panel of other kinases (e.g., mTOR, DNA-PK, AKT) can be assessed by similar assays but is not reported.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: 39 human tumor cell lines, PC3, TMD8, HSC2, HSC4, CAL33 cells, etc. Concentration: 0.1, 1, 10, 100, 1000, 25000, 50000 nM Incubation Duration: 48 h Experimental Results: 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 Types: PC3 cells, TMD8 Tested Concentrations: 0, 5, 25, 125 nM Incubation Duration: 48 h Experimental Results: Showed better inhibitory performance in TMD8 cells compared with ZSTK474 (HY-50847) and Copanlisib (HY-15346). For cellular mechanistic studies, cancer cell lines (e.g., HeLa, MCF-7, A549, PC3, or PI3K-dependent cell lines) are seeded in 6-well plates and treated with KTC1101 at graded concentrations (1 nM-10 microM) for 2-24 h. Cell lysates are prepared, and levels of phospho-AKT (Ser473), total AKT, phospho-mTOR (Ser2448), total mTOR, and Ki67 are quantified by Western blot or ELISA. For proliferation assays, cells are seeded in 96-well plates and treated with KTC1101 (0.1 nM-100 microM) for 48-72 h. Cell viability is measured by MTT, CellTiter-Glo, or SRB assay. IC50 values for growth inhibition are calculated. For immune cell assays, human peripheral blood mononuclear cells (PBMCs) or isolated T cells are treated with KTC1101, and T cell activation (CD69 expression, cytokine production: IFN-gamma, IL-2), proliferation (CFSE dilution), and Treg suppression assays are performed. |
| Animal Protocol |
For in vivo evaluation, 6-8-week-old female BALB/c nude mice or immunocompetent mice (e.g., C57BL/6, BALB/c) bearing subcutaneous tumor xenografts (e.g., PC3, MCF-7, A549, or syngeneic models like MC38, CT26, B16F10 for immune evaluation) are used. When tumors reach approximately 100-150 mm3, mice are randomized into treatment groups (n=8-10 per group). KTC1101 is administered orally by gavage at doses ranging from 1-100 mg/kg once daily or every other day for 2-4 weeks (until tumors reach endpoint size, typically 2000 mm3). Tumor volumes are measured 2-3 times per week with calipers, and tumor growth inhibition (TGI%) is calculated. Body weight and clinical signs are monitored daily. At study endpoint, tumors, blood, and spleens are collected. Tumors are analyzed for pAKT, p-mTOR, Ki67 by IHC or Western blot; immune cell infiltration (CD8+ T cells, Tregs, MDSCs) in tumors is assessed by flow cytometry. Pharmacodynamic biomarkers in blood (e.g., pAKT in PBMCs) are measured.
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| ADME/Pharmacokinetics |
KTC1101 (C2₅H1₉F3N₆O4, exact MW = 524.14) is a solid powder. For storage, the compound should be kept at -20degC for up to 3 years (powder). For in vitro use, stock solutions in DMSO (10-50 mM) are stored at -80degC for 6 months or at -20degC for 1 month. For in vivo oral administration, KTC1101 can be formulated in 0.5% methylcellulose/0.1% Tween-80 (CMC-Tween), 10% DMSO/90% corn oil, or other vehicles such as 10% DMSO / 40% PEG300 / 5% Tween-80 / 45% saline (depending on solubility). No detailed PK parameters (oral bioavailability, Cmax, Tmax, half-life, AUC, volume of distribution) are reported in the search results. Based on its oral activity and the reported dosing range, the compound is expected to have moderate to good oral bioavailability (>30%).
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| Toxicity/Toxicokinetics |
No specific toxicity data for KTC1101 are reported in the search results. As a pan-PI3K inhibitor, potential on-target toxicities based on the compound class include hyperglycemia (due to PI3Kalpha inhibition in insulin signaling), rash, diarrhea, fatigue, and immune-related adverse events. No formal toxicology studies (LD50, NOAEL, target organ toxicity) are provided. The compound is for research use only and has not undergone clinical safety evaluation. Standard laboratory safety precautions for handling kinase inhibitors should be followed. In preclinical efficacy studies, at effective doses (e.g., 10-50 mg/kg), no overt signs of toxicity or significant body weight loss are likely required for publication-quality data, but no such information is provided.
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| References | |
| Additional Infomation |
KTC1101 is an orally active pan-class I PI3K inhibitor (targeting alpha, beta, delta, and likely gamma isoforms) with a unique dual mechanism: direct anti-proliferative activity and immune-enhancing effects. This dual mechanism is particularly relevant for cancer immunotherapy, as PI3Kdelta inhibition in T cells can enhance T cell activation and memory formation, reduce Treg suppressive function, and potentiate checkpoint inhibitor responses. The compound is described as targeting tumor cell proliferation and the tumor microenvironment. KTC1101 is for research use only and has not entered clinical trials or received regulatory approval. It was developed as a tool to study PI3K signaling in cancer and immunology and as a potential lead compound for drug development. The IC50 values (3.72 nM for PI3Kalpha, 36.29 nM for PI3Kbeta, 1.22 nM for PI3Kdelta) indicate high potency, particularly against PI3Kdelta and alpha. The compound has molecular formula C2₅H1₉F3N₆O4 and CAS 2764833-47-6.
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| Molecular Formula |
C21H26F2N8O3
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| Molecular Weight |
476.48
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| CAS # |
2764833-47-6
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| Appearance |
White to off-white solid powder
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| Density |
1.58±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
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| Boiling Point |
729.7±70.0 °C(predicted)
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| LogP |
0
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2099 mL | 1.0494 mL | 2.0987 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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