ZD-2767P
Based on 1 Customer Validation
ZD-2767P is a key prodrug in the antibody-directed enzyme prodrug therapy (ADEPT) system. The mechanism of action of ZD-2767Prelies entirely on the ADEPT strategy and proceeds in two steps: first, ZD2767C is administered, which locally enriches carboxypeptidase G2 at tumor sites; then, the prodrug ZD-2767P is administered, which is specifically recognized by the locally enriched carboxypeptidase G2, with its carbamate bond hydrolyzed to release the active drug ZD2767D. ZD-2767P can be used in research related to clear cell renal cell carcinoma, colorectal cancer and colon cancer.
For research use only. We do not sell to patients.
- CAS No.: 156079-88-8
- Formula: C16H20I2N2O6
- Molecular Weight:590.15
-
Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| LoVo | IC50 |
47.2 μM
Compound: 1b
|
Cytotoxicity against colorectal tumor cell line LoVo 1 hour after incubation.
Cytotoxicity against colorectal tumor cell line LoVo 1 hour after incubation.
|
[PMID: 8544182] |
In Vitro
ZD-2767P (1 h incubation; 3 days post-wash culture) has low inherent cytotoxicity against LoVo colorectal tumor cells (IC50 = 47 ± 31 μM), but when cleaved by CPG2, releases a metabolite with potent cytotoxicity against these cells (IC50 = 0.32 ± 0.28 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Athymic nude mice (nu/nu: Alpk, outbred)[2]
-
Dosage:3 × 70 mg/kg; 3 × 62 mg/kg; 3 × 52 mg/kg; 3 × 90 mg/kg; 3 × 90 mg/kg + 0.5 mg/kg ZD2767C
-
Administration:i.p.; three hourly injections over a 2-hour period; administered 72 hours after ZD2767C
-
Result:Induced complete macroscopic regression in 50% (22 of 39) of tumors, with tumors later reappearing in most cases.
Produced tumor growth delays of 33 days (3 × 70 mg/kg), 37 days (3 × 62 mg/kg), 32 days (3 × 52 mg/kg), 20 days (3 × 90 mg/kg), and 16 days (3 × 90 mg/kg with 0.5 mg/kg ZD2767C).
Caused 7-10% body-weight loss across doses.
Showed no antitumor activity when administered alone.
Chemical Information
-
CAS No. 156079-88-8
-
Appearance Solid
-
Molecular Weight 590.15
-
Formula C16H20I2N2O6
-
Color Light yellow to yellow
-
SMILES
O=C(O)CC[C@@H](C(O)=O)NC(OC1=CC=C(N(CCI)CCI)C=C1)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
In Vitro:
DMSO : 25 mg/mL (42.36 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 (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 (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)
Purity & Documentation
-
Data Sheet (280 KB)
-
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)
-
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 (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 | 1.6945 mL | 8.4724 mL | 16.9448 mL | 42.3621 mL |
| 5 mM | 0.3389 mL | 1.6945 mL | 3.3890 mL | 8.4724 mL | |
| 10 mM | 0.1694 mL | 0.8472 mL | 1.6945 mL | 4.2362 mL | |
| 15 mM | 0.1130 mL | 0.5648 mL | 1.1297 mL | 2.8241 mL | |
| 20 mM | 0.0847 mL | 0.4236 mL | 0.8472 mL | 2.1181 mL | |
| 25 mM | 0.0678 mL | 0.3389 mL | 0.6778 mL | 1.6945 mL | |
| 30 mM | 0.0565 mL | 0.2824 mL | 0.5648 mL | 1.4121 mL | |
| 40 mM | 0.0424 mL | 0.2118 mL | 0.4236 mL | 1.0591 mL |