CDD-2807
Based on 1 Customer Validation
CDD-2807 is a blood-testis barrier-penetrant STK33 inhibitor (Kd = 0.02 nM). CDD-2807 acts by impairing sperm motility and hyperactivation, while inhibiting off-target kinases such as CLK4 (Kd = 0.9 nM), CLK2 (Ki = 1.3 nM), RET (Ki = 0.3 nM), and CLK1 (Ki = 3.1 nM). CDD-2807 can be used in research on reversible male contraception.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.52%
- CAS. Nr.: 3086536-23-1
- Formel: C29H26N4O
- Molecular Weight:446.54
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
STK33 9.2 nM (IC50) |
STK33 0.02 nM (Kd) |
CLK4 85 nM (IC50) |
CLK4 0.9 nM (Ki) |
CLK2 101 nM (IC50) |
CLK2 1.3 nM (Ki) |
CLK1 116 nM (IC50) |
CLK1 3.1 nM (Ki) |
Ret 363 nM (IC50) |
Ret 0.3 nM (Ki) |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
9.2 nM
|
Intracellular kinase target engagement IC50 against STK33 in HEK293 cells by NanoBRET assay.
Intracellular kinase target engagement IC50 against STK33 in HEK293 cells by NanoBRET assay.
|
38781365 |
| HEK293 | IC50 |
85 nM
|
Intracellular kinase target engagement IC50 against CLK4 in HEK293 cells by NanoBRET assay.
Intracellular kinase target engagement IC50 against CLK4 in HEK293 cells by NanoBRET assay.
|
38781365 |
| HEK293 | IC50 |
101 nM
|
Intracellular kinase target engagement IC50 against CLK2 in HEK293 cells by NanoBRET assay.
Intracellular kinase target engagement IC50 against CLK2 in HEK293 cells by NanoBRET assay.
|
38781365 |
| HEK293 | IC50 |
363 nM
|
Intracellular kinase target engagement IC50 against RET in HEK293 cells by NanoBRET assay.
Intracellular kinase target engagement IC50 against RET in HEK293 cells by NanoBRET assay.
|
38781365 |
| HEK293 | IC50 |
116 nM
|
Intracellular kinase target engagement IC50 against CLK1 in HEK293 cells by NanoBRET assay.
Intracellular kinase target engagement IC50 against CLK1 in HEK293 cells by NanoBRET assay.
|
38781365 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
CDD-2807 (50 mg/kg; once daily; 21 days) induces a reversible contraceptive effect in male mice with functional and morphologic sperm defects[1].
CDD-2807 (50 mg/kg/day; 7 days) reduces sperm motility parameters without altering testis size or sperm counts in male mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:mice[1]
-
Dosage:15 mg/kg
-
Administration:intraperitoneally; twice per day; 21 days
-
Result:In month 1, 4 of 6 males sired litters; the cohort produced 1.0 litters per male and 0.92 pups per female per litter.
In month 2, no litters were produced by females housed with males.
Sperm motility, progressive sperm, and hyperactivated sperm were reduced in mice.
Testis size of mice was unchanged.
Histologically, testes and epididymis of mice showed no detectable defects.
After dosing was halted at day 63, three previously dosed cohort males sired offspring within the first month (7.67 pups per litter per female).
-
Animal Model:mice[1]
-
Dosage:50 mg/kg
-
Administration:once per day; 21 days
-
Result:In month 1, only one female became pregnant and delivered a single pup from the seven males (0.07 pups per litter per female).
In month 2, males did not sire any litters.
Sperm counts, sperm motility, progressive sperm, and hyperactivated sperm were reduced in mice.
Testis size of mice was unchanged.
Histology showed round spermatids in the epididymis, and scanning electron microscopy demonstrated teratozoospermia.
After dosing, mice took 53.5 days to sire their first litters.
-
Animal Model:mice[1]
-
Dosage:50 mg/kg/day
-
Administration:daily; 7 days
-
Result:Testis size and sperm counts were not altered in mice.
Sperm motility, progressive sperm, and sperm hyperactivation were reduced in mice.
Chemical Information
-
CAS. Nr. 3086536-23-1
-
Appearance Solid
-
Molecular Weight 446.54
-
Formel C29H26N4O
-
Color White to off-white
-
SMILES
O=C(C1=CC2=C(NN=C2C#CC3=CC=CC=C3C4=CC=CC=C4)C=C1)N5CC6(CNCCC6)C5
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (111.97 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.60 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Reinheit & Dokumentation
-
Data Sheet (285 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
Verweise
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 | 2.2394 mL | 11.1972 mL | 22.3944 mL | 55.9860 mL |
| 5 mM | 0.4479 mL | 2.2394 mL | 4.4789 mL | 11.1972 mL | |
| 10 mM | 0.2239 mL | 1.1197 mL | 2.2394 mL | 5.5986 mL | |
| 15 mM | 0.1493 mL | 0.7465 mL | 1.4930 mL | 3.7324 mL | |
| 20 mM | 0.1120 mL | 0.5599 mL | 1.1197 mL | 2.7993 mL | |
| 25 mM | 0.0896 mL | 0.4479 mL | 0.8958 mL | 2.2394 mL | |
| 30 mM | 0.0746 mL | 0.3732 mL | 0.7465 mL | 1.8662 mL | |
| 40 mM | 0.0560 mL | 0.2799 mL | 0.5599 mL | 1.3997 mL | |
| 50 mM | 0.0448 mL | 0.2239 mL | 0.4479 mL | 1.1197 mL | |
| 60 mM | 0.0373 mL | 0.1866 mL | 0.3732 mL | 0.9331 mL | |
| 80 mM | 0.0280 mL | 0.1400 mL | 0.2799 mL | 0.6998 mL | |
| 100 mM | 0.0224 mL | 0.1120 mL | 0.2239 mL | 0.5599 mL |
CDD-2807 Related Classifications
HY-162565 Related Classifications
Powered by Bioz