EC1169
Based on 1 Customer Validation
EC1169 is a cytotoxic maytansinoid conjugate that specifically binds to prostate-specific membrane antigen (PSMA). EC1169 precisely delivers the maytansinoid B hydrazide payload to PSMA-positive cells to exert antitumor activity. EC1169 only inhibits the growth of PSMA-positive cells but has no effect on PSMA-negative cells, and enables complete recovery in mice bearing PSMA-positive tumors. EC1169 exhibits safety with no body weight loss or major organ damage induced. EC1169 is used in studies of prostate cancer and other PSMA-expressing malignancies.
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- Purity: 98.06%
- CAS No.: 1610413-96-1
- 화학식: C78H112N14O28S3
- 분자량:1790.00
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보관:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
Biological Activity
The binding affinity of EC1169 to PSMA on LNCaP cells is 6.5-fold that of the reference ligand PMPA[3].
EC1169 (1 μM; 2 h pulsed treatment+72 h) inhibits the growth of PSMA-positive LNCaP cells with an IC50 of approximately 13 nM, but shows no activity against PSMA-negative A549 and KB cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PSMA-positive LNCaP cells, PSMA-negative A549 cells, PSMA-negative KB cells
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Concentration:up to 1 μM
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Incubation Time:2 h (pulse); 72 h (chase)
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Result:Inhibited the growth of PSMA-positive LNCaP cells with an in vitro IC50 of ~13 nM.
Induced membrane blebbing, loss of membrane integrity, and cell death within 24 h.
Showed no activity against PSMA-negative A549 and KB cells.
EC1169 (2 μmol/kg; i.v.; 3 times per week; 2 weeks) produces 100% complete responses in nu/nu mice bearing PSMA-positive LNCaP xenografts, with 29% of mice remaining tumor-free at 90 days, and no associated weight loss[3].
EC1169 (2 μmol/kg; i.v.; 3 times per week; 5 doses) exhibits no anti-tumor activity in nu/nu mice bearing PSMA-negative KB xenografts, confirming its PSMA-dependent specificity[3].
EC1169 (2 μmol/kg; i.v.; 3 times per week; 2 weeks per cycle; repeated for a second 2-week cycle after a 3-week drug holiday) produces a 100% partial response rate in nu/nu mice bearing PSMA-positive MDA-PCa 2b xenografts after one treatment cycle, and a combined 50% partial and 50% complete response rate after a second cycle, with no associated weight loss[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:nu/nu (nude) mice with Cervical cancer (female, 4-8 weeks old, subcutaneous inoculation with PSMA-negative KB human cervical cancer cells)[3]
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Dosage:2 μmol/kg
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Administration:i.v.; three times per week; 5 doses
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Result:Showed no anti-tumor activity against PSMA-negative KB xenografts.
Resulted in tumor growth comparable to untreated controls.
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Animal Model:nu/nu (nude) mice with Prostate cancer (male, 4-8 weeks old, subcutaneous inoculation with PSMA-positive MDA-PCa 2b human prostate cancer cells mixed with Matrigel)[3]
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Dosage:2 μmol/kg
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Administration:i.v.; three times per week; 2 weeks per cycle; repeated for a second 2-week cycle after a 3-week drug holiday
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Result:Produced a 100% partial response rate after the first 2-week treatment cycle, with tumors regressing but recurring in all mice by post-tumor implant day 56.
Yielded a 50% partial response rate and 50% complete response rate by post-tumor implant day 68 after the second 2-week cycle.
Caused no significant weight loss with either treatment cycle.
Chemical Information
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CAS No. 1610413-96-1
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Appearance Solid
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분자량 1790.00
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화학식 C78H112N14O28S3
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Color White to off-white
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SMILES
O=C([C@@H]1N(CCCC1)C)N[C@@H]([C@@H](C)CC)C(N(COC(CCC)=O)[C@@H](C(C)C)C[C@H](C2=NC(C(N[C@H](C[C@H](C)C(NNC(OCCSSC[C@@H](C(O)=O)NC([C@H](CC(O)=O)NC([C@H](CC(O)=O)NC(CC3=CC=C(C=C3)CNC(NCCCC[C@@H](C(O)=O)NC(N[C@H](C(O)=O)CCC(O)=O)=O)=O)=O)=O)=O)=O)=O)CC4=CC=C(C=C4)O)=O)=CS2)OC(C)=O)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
용액&용해도
DMSO : 100 mg/mL (55.87 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
순도&문서
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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 (protect from light, stored under nitrogen). 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 | 0.5587 mL | 2.7933 mL | 5.5866 mL | 13.9665 mL |
| 5 mM | 0.1117 mL | 0.5587 mL | 1.1173 mL | 2.7933 mL | |
| 10 mM | 0.0559 mL | 0.2793 mL | 0.5587 mL | 1.3966 mL | |
| 15 mM | 0.0372 mL | 0.1862 mL | 0.3724 mL | 0.9311 mL | |
| 20 mM | 0.0279 mL | 0.1397 mL | 0.2793 mL | 0.6983 mL | |
| 25 mM | 0.0223 mL | 0.1117 mL | 0.2235 mL | 0.5587 mL | |
| 30 mM | 0.0186 mL | 0.0931 mL | 0.1862 mL | 0.4655 mL | |
| 40 mM | 0.0140 mL | 0.0698 mL | 0.1397 mL | 0.3492 mL | |
| 50 mM | 0.0112 mL | 0.0559 mL | 0.1117 mL | 0.2793 mL |
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