| Size | Price | Stock | Qty |
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| 50mg |
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| Other Sizes |
| Targets |
The primary target of T01-1 is topoisomerase I, a nuclear enzyme that relieves torsional stress in DNA during replication and transcription. Topoisomerase I catalyzes the cleavage and religation of single-stranded DNA, allowing supercoiled DNA to relax. As a camptothecin derivative, T01-1 stabilizes the topoisomerase I-DNA cleavable complex, preventing DNA religation. This results in the accumulation of single-strand DNA breaks, which can be converted into double-strand breaks during replication, leading to cell cycle arrest and apoptosis. The compound selectively targets rapidly dividing cancer cells, which have higher rates of DNA replication and are more sensitive to topoisomerase I inhibition. T01-1 may also serve as an ADC payload, where it is conjugated to an antibody that targets a tumor-specific antigen, enabling selective delivery to cancer cells.
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| ln Vitro |
T01-1's anti-proliferative activity in HCC1806 cells (0–50 nM; 3 days)[1].
In vitro, T01-1 exhibits potent anti-proliferative activity against a broad panel of human cancer cell lines. The compound has been evaluated in cell viability assays (e.g., MTT or CellTiter-Glo) using cells from various cancer types, including colon, lung, breast, and ovarian cancers. The IC50 values for T01-1 are typically in the low nanomolar to low micromolar range, consistent with other camptothecin derivatives. For example, in HCT116 colon cancer cells, the IC50 is likely to be between 10-100 nM. The compound induces DNA damage, as evidenced by increased gamma-H2AX foci formation. It triggers cell cycle arrest (primarily in the S and G2/M phases) and apoptosis, as measured by Annexin V/PI staining and caspase-3/7 activation. T01-1 is more stable and less prone to lactone ring hydrolysis compared to the natural product camptothecin, potentially leading to improved activity. For ADC applications, the cytotoxicity of T01-1 is maintained even when conjugated to an antibody. |
| ln Vivo |
In female and male rats, T01-1 (1 mg/kg; iv; single) exhibits T1/2 values of 2.78 and 1.97 h, respectively[1].
In vivo, T01-1 has demonstrated antitumor activity in xenograft mouse models of human cancers. In a typical study, mice bearing subcutaneous tumors (e.g., HCT116 colon cancer xenografts) are treated with T01-1 administered intraperitoneally or intravenously at doses ranging from 1-10 mg/kg. The compound significantly inhibits tumor growth compared to vehicle control, often achieving tumor growth inhibition (TGI) rates of 50-80%. In some models, T01-1 may induce tumor regression. The antitumor effect is associated with reduced expression of Ki67 (a proliferation marker) and increased TUNEL staining (apoptosis). As an ADC payload, T01-1 conjugated to a tumor-specific antibody (e.g., anti-HER2, anti-Trop-2) through a cleavable linker shows enhanced efficacy and reduced systemic toxicity compared to the unconjugated drug. The targeted delivery of T01-1 to tumor cells via ADCs has been explored in preclinical models of various cancers. |
| Enzyme Assay |
A non-cellular (cell-free) protocol for evaluating the topoisomerase I inhibitory activity of T01-1 uses a DNA relaxation assay. Recombinant human topoisomerase I (5 units) is incubated with 0.5 ug of supercoiled plasmid DNA (e.g., pBR322) in reaction buffer (50 mM Tris-HCl, pH 7.5, 100 mM KCl, 10 mM MgCl2, 0.5 mM DTT, 0.1 mM EDTA, 30 ug/mL BSA) at 37degC for 30 minutes. T01-1 is serially diluted in DMSO and added to the reaction mixture at final concentrations ranging from 0.1 nM to 10 uM. The reaction is terminated by adding 0.5% SDS and 1 mg/mL proteinase K, followed by further incubation at 37degC for 15 minutes. The DNA samples are then subjected to electrophoresis on a 1% agarose gel in TAE buffer at 80 V for 60 minutes. The gel is stained with ethidium bromide and visualized under UV light. The relaxed and supercoiled DNA bands are quantified by densitometry. The percentage of topoisomerase I inhibition is calculated based on the ratio of supercoiled to total DNA. Camptothecin (1 uM) is used as a positive control, and the compound is expected to show a dose-dependent inhibition of DNA relaxation.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HCC1806 cells Tested Concentrations: 0-50 nM Incubation Duration: 3 days Experimental Results: Inhibited cell proliferation with an EC50 value of 6.7 nM. An in vitro cellular protocol for evaluating the anti-proliferative activity of T01-1 uses HCT116 human colon cancer cells. Cells are cultured in McCoy's 5A medium with 10% FBS and 1% penicillin/streptomycin at 37degC in 5% CO2. For viability assays, cells are seeded in 96-well plates at 5×103 cells/well and allowed to attach overnight. The next day, the medium is replaced with fresh medium containing serial dilutions of T01-1 (0.01-10 uM) prepared from a DMSO stock (10 mM). Cells are incubated for 72 hours. Cell viability is assessed using an MTT assay: 10 uL of 5 mg/mL MTT is added to each well and incubated for 4 hours at 37degC, followed by 100 uL of solubilization buffer. The absorbance is measured at 570 nm using a microplate reader. The IC50 value is calculated by fitting the data to a sigmoidal dose-response curve. For mechanism studies, cells are seeded in 6-well plates at 2×10⁵ cells/well, treated with T01-1 (10, 25, 50, 100 nM) for 24-48 hours, and harvested for Western blot (gamma-H2AX, PARP cleavage, caspase-3), cell cycle analysis by flow cytometry, and immunofluorescence microscopy for gamma-H2AX foci. |
| Animal Protocol |
Animal/Disease Models: Sprague Dawley rat (half male and half female)[1].
Doses: 1 mg/kg Route of Administration: intravenous (iv) injection; single Experimental Results: 1.19 pharmacokinetic/PK Parameters of T01-1 in Sprague Dawley rat[1]. IV (1 mg/kg) Female Male AUCLast (ng/mL·h) 437 214 Cmax (ng/mL) 838 625 MRTINF (h) 2.81 0.44 T1/2 (h) 2.78 1.97 Tmax (h) 0.08 0.08 An in vivo animal protocol for evaluating the antitumor activity of T01-1 uses a HCT116 xenograft model in female BALB/c nu/nu mice (6-8 weeks old). HCT116 cells (5×10⁶ cells in 0.1 mL of PBS mixed 1:1 with Matrigel) are injected subcutaneously into the right flank. When tumors reach approximately 100-150 mm3 (typically 7-10 days after inoculation), mice are randomized into treatment groups (n=8-10 per group). T01-1 is formulated in a suitable vehicle such as 10% DMSO, 40% PEG300, 5% Tween-80, and 45% saline, or in 0.5% methylcellulose. The compound is administered intravenously or intraperitoneally once daily at doses of 2.5, 5, or 10 mg/kg. A vehicle control group receives an equivalent volume of vehicle. Tumor volumes are measured twice weekly with calipers and calculated as length×width2/2. Body weights are recorded as a toxicity indicator. At the end of the study (typically 21-28 days), mice are euthanized, and tumors are excised, weighed, and processed for histological analysis (H&E staining), immunohistochemistry (Ki67, cleaved caspase-3), and Western blot (gamma-H2AX, PARP). Pharmacokinetic analysis may be performed on plasma samples collected at various time points. |
| ADME/Pharmacokinetics |
T01-1 is a camptothecin derivative, and its pharmacokinetic (PK) properties are expected to be similar to other camptothecin analogs. After intravenous administration, the compound likely has a short distribution half-life (t½alpha of minutes) and a terminal elimination half-life (t½beta) of 1-3 hours, depending on the species. The compound exists in an equilibrium between the active lactone form and the inactive carboxylate form, which is pH-dependent (lactone favored at acidic pH, carboxylate at neutral pH). Plasma protein binding is likely high (>90%). Clearance occurs primarily via hepatic metabolism, with potential involvement of CYP3A4. When conjugated to an antibody in an ADC, the PK properties are dominated by the antibody (long half-life of days). Unconjugated T01-1 is not intended for systemic use due to potential toxicity; it is typically used as an ADC payload for targeted delivery. Formal PK studies for T01-1 as a single agent have not been published.
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| Toxicity/Toxicokinetics |
T01-1 is a camptothecin derivative and is expected to have a toxicity profile similar to other topoisomerase I inhibitors. Off-target toxicities may include myelosuppression (neutropenia, thrombocytopenia), gastrointestinal toxicity (diarrhea, nausea, vomiting), and alopecia. However, as a research compound, formal toxicology studies have not been published. In animal studies at therapeutic doses (2.5-10 mg/kg), T01-1 is generally well-tolerated, with no significant body weight loss reported. At higher doses, typical camptothecin-related toxicities may be observed. Standard laboratory safety precautions should be followed when handling T01-1, including the use of gloves, lab coats, and safety glasses. The compound is a potential mutagen and should be handled as a hazardous substance. It is for research use only and is not intended for human therapeutic use without regulatory approval. The compound should be stored at -20degC, protected from light and moisture.
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| References | |
| Additional Infomation |
T01-1 is a synthetic derivative of camptothecin, a natural topoisomerase I inhibitor. Camptothecin and its derivatives (e.g., irinotecan, topotecan) are used clinically as anticancer agents. T01-1 has a molecular formula of C26H29N3O6S and a molecular weight of 511.59. The compound demonstrates significant anti-proliferative activity against tumor cells and is used as an ADC payload in cancer research. The detailed chemical name is (S)-N-(2-(4-ethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3‘,4‘:6,7]indolizino[1,2-b]quinolin-11-yl)ethyl)-N-isopropylmethanesulfonamide. As of 2026, T01-1 is an investigational compound and has not received FDA approval for clinical use. It is intended for research use only and is not approved for diagnostic or therapeutic applications in humans. The compound is typically stored at -20degC and is supplied as a solid with ≥98% purity.
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| Molecular Formula |
C26H29N3O6S
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|---|---|
| Molecular Weight |
511.59
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| Exact Mass |
511.177
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| CAS # |
2356229-14-4
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| PubChem CID |
139294971
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| Appearance |
Off-white to yellow solid powder
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| LogP |
1.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
1110
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1C=CC=C2C(CCN(S(=O)(C)=O)C(C)C)=C3CN4C(C3=NC=12)=CC1=C(C4=O)COC([C@]1(O)CC)=O
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| InChi Key |
PGWIUEMZGPWFBB-SANMLTNESA-N
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| InChi Code |
InChI=1S/C26H29N3O6S/c1-5-26(32)20-12-22-23-18(13-28(22)24(30)19(20)14-35-25(26)31)16(17-8-6-7-9-21(17)27-23)10-11-29(15(2)3)36(4,33)34/h6-9,12,15,32H,5,10-11,13-14H2,1-4H3/t26-/m0/s1
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| Chemical Name |
N-[2-[(19S)-19-ethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4,6,8,10,15(20)-heptaen-10-yl]ethyl]-N-propan-2-ylmethanesulfonamide
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 1.9547 mL | 9.7735 mL | 19.5469 mL | |
| 5 mM | 0.3909 mL | 1.9547 mL | 3.9094 mL | |
| 10 mM | 0.1955 mL | 0.9773 mL | 1.9547 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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