LDR102
Based on 1 Customer Validation
LDR102 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. LDR102 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. LDR102 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.78%
- CAS No.: 3053223-31-4
- 화학식: C33H27N5O3
- 분자량:541.60
-
보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
Ki: 0.10 μM (ROR1)
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
1.37 μM
Compound: 19h
|
Antiproliferative activity against human A549 cells harboring high ROR1 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells harboring high ROR1 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 38913699] |
| MDA-MB-231 | IC50 |
0.47 μM
Compound: 19h
|
Antiproliferative activity against human MDA-MB-231 cells harboring high ROR1 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells harboring high ROR1 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 38913699] |
| NCI-H1975 | IC50 |
0.36 μM
Compound: 19h
|
Antiproliferative activity against human NCI-H1975 cells harboring high ROR1 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells harboring high ROR1 expression assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 38913699] |
Chemical Information
-
CAS No. 3053223-31-4
-
Appearance Solid
-
분자량 541.60
-
화학식 C33H27N5O3
-
Color Light yellow to yellow
-
SMILES
CN(C=C1C2=CC=C(OCOC)C=C2)C3=C1C=CC(NC(C4=CC(C#CC5=CC=NC6=C5C=NN6)=C(C)C=C4)=O)=C3
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
DMSO : 100 mg/mL (184.64 mM; ultrasonic and warming and heat to 60°C; 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). 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). 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 (4.62 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
-
Data Sheet (272 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)
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). 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 | 1.8464 mL | 9.2319 mL | 18.4638 mL | 46.1595 mL |
| 5 mM | 0.3693 mL | 1.8464 mL | 3.6928 mL | 9.2319 mL | |
| 10 mM | 0.1846 mL | 0.9232 mL | 1.8464 mL | 4.6160 mL | |
| 15 mM | 0.1231 mL | 0.6155 mL | 1.2309 mL | 3.0773 mL | |
| 20 mM | 0.0923 mL | 0.4616 mL | 0.9232 mL | 2.3080 mL | |
| 25 mM | 0.0739 mL | 0.3693 mL | 0.7386 mL | 1.8464 mL | |
| 30 mM | 0.0615 mL | 0.3077 mL | 0.6155 mL | 1.5387 mL | |
| 40 mM | 0.0462 mL | 0.2308 mL | 0.4616 mL | 1.1540 mL | |
| 50 mM | 0.0369 mL | 0.1846 mL | 0.3693 mL | 0.9232 mL | |
| 60 mM | 0.0308 mL | 0.1539 mL | 0.3077 mL | 0.7693 mL | |
| 80 mM | 0.0231 mL | 0.1154 mL | 0.2308 mL | 0.5770 mL | |
| 100 mM | 0.0185 mL | 0.0923 mL | 0.1846 mL | 0.4616 mL |