TH1338
Based on 1 Customer Validation
TH1338 (compound 3b), an orally active camptothecin derivative and a potent chemotherapeutic agent for cancer, demonstrates excellent cytotoxic potency against human tumor cell lines in vitro. TH1338 (compound 3b) possesses significant brain penetration, favorable efflux pump properties, and hematological toxicity profile.
For research use only. We do not sell to patients.
- Purity: 98.77%
- CAS No.: 1258494-60-8
- Formula: C22H21N3O4
- Molecular Weight:391.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
7 nM
Compound: 3b
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Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay
Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| Bone marrow cell | IC50 |
110 nM
Compound: 3b
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Cytotoxicity against mouse bone marrow cell by CFU-GM assay
Cytotoxicity against mouse bone marrow cell by CFU-GM assay
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[PMID: 21341674] |
| Bone marrow cell | IC50 |
620 nM
Compound: 3b
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Cytotoxicity against human bone marrow cell by CFU-GM assay
Cytotoxicity against human bone marrow cell by CFU-GM assay
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[PMID: 21341674] |
| DU-145 | IC50 |
1200 nM
Compound: 3b
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Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay
Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| H69AR | IC50 |
240 nM
Compound: 3b
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Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay
Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| HT-29 | IC50 |
300 nM
Compound: 3b
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Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay
Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| IGROV-1 | IC50 |
20 nM
Compound: 3b
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Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay
Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| LNCaP | IC50 |
120 nM
Compound: 3b
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Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay
Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| Malme-3M | IC50 |
1200 nM
Compound: 3b
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Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay
Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| MES-SA | IC50 |
4 nM
Compound: 3b
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Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay
Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| MES-SA/Dx5 | IC50 |
12 nM
Compound: 3b
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Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay
Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| NCI-H460 | IC50 |
120 nM
Compound: 3b
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Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA
Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA
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[PMID: 21341674] |
| NCI-H69 | IC50 |
110 nM
Compound: 3b
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Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay
Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| PC-3 | IC50 |
24 nM
Compound: 3b
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Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay
Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
| SK-MEL-2 | IC50 |
130 nM
Compound: 3b
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Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay
Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay
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[PMID: 21341674] |
TH1338 (compound 3b) demonstrates significant brain penetration when dosed orally in mice[1].
TH1338 (compound 3b) exhibits potent anti-tumor activity in H460 (NSCLC) human tumor xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H460 (NSCLC) human tumor xenograft model.
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Concentration:40 mg/kg.
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Incubation Time:Oral gavage.
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Result:Exhibited superior antitumor activity.
Chemical Information
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CAS No. 1258494-60-8
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Appearance Solid
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Molecular Weight 391.42
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Formula C22H21N3O4
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Color Light yellow to yellow
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SMILES
O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=C(CC)C5=CC=CC=C5N=C4C3=C2N)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 10 mg/mL (25.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.82 mg/mL (4.65 mM); Clear solution
This protocol yields a clear solution of ≥ 1.82 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (18.2 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (279 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Jian-Xin Duan, et al. 14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment. J Med Chem. 2011 Mar 24;54(6):1715-23. [Content Brief]
[2]. Xia Cheng, et al. Preparation, Characterization, and In Vivo Study of 7-Ethyl-14-Aminocamptothecin-Loaded Poly(Ethylene Glycol)2000 -Poly(Lactic Acid)2000 Polymeric Micelles Against H460 Human Nonsmall Cell Lung Carcinoma. J Pharm Sci. 2015 Nov;104(11):3934-3942. [Content Brief]
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 | 2.5548 mL | 12.7740 mL | 25.5480 mL | 63.8700 mL |
| 5 mM | 0.5110 mL | 2.5548 mL | 5.1096 mL | 12.7740 mL | |
| 10 mM | 0.2555 mL | 1.2774 mL | 2.5548 mL | 6.3870 mL | |
| 15 mM | 0.1703 mL | 0.8516 mL | 1.7032 mL | 4.2580 mL | |
| 20 mM | 0.1277 mL | 0.6387 mL | 1.2774 mL | 3.1935 mL | |
| 25 mM | 0.1022 mL | 0.5110 mL | 1.0219 mL | 2.5548 mL |
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