2. Immunology/Inflammation
  3. PSMA
  4. EC1169

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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EC1169

EC1169 Chemical Structure

CAS No. : 1610413-96-1

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EC1169 Related Antibodies

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Description

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[1][2][3].

In Vitro

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.

EC1169 Related Antibodies

Cell Viability Assay[3]

Cell Line: PSMA-positive LNCaP cells, PSMA-negative A549 cells, PSMA-negative KB cells
Concentration: up to 1 μM
Incubation Time: 2 h (pulse); 72 h (chase)
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.
In Vivo

EC1169 demonstrated significantly greater antitumor activity against PSMA-positive human prostate cancer xenografts than Docetaxel (HY-B0011); at 90 days post-transplantation, all tumor-bearing mice achieved complete remission with no observed toxicity[1].
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.

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]
Dosage: 2 μmol/kg
Administration: i.v.; three times per week; 5 doses
Result: Showed no anti-tumor activity against PSMA-negative KB xenografts.
Resulted in tumor growth comparable to untreated controls.
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]
Dosage: 2 μmol/kg
Administration: i.v.; three times per week; 2 weeks per cycle; repeated for a second 2-week cycle after a 3-week drug holiday
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.
Molecular Weight

1790.00

Formula

C78H112N14O28S3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5587 mL 2.7933 mL 5.5866 mL
5 mM 0.1117 mL 0.5587 mL 1.1173 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
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:
%
DMSO +
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EC11691610413-96-1EC 1169EC-1169PSMAProstate-specific membrane antigenPSMA-positive human xenograftsPSMA-positive cellsPSMA-expressing cancerPSMA-negative cellstubulysin B hydrazideL-Glu-urea-L-LysA549 cellsLNCaP cellsprostate cancernude miceInhibitorinhibitorinhibit

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