SEL24-B489
Based on 1 Customer Validation
SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.02%
- No. CAS: 1616359-00-2
- Fòrmula: C15H18Br2N4O2
- Peso molecular:446.14
-
Almacenamiento: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]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
HY-15604
AZD1208PIM Inhibitor -
HY-101126
NuvisertibPIM Kinase Inhibitor -
HY-12432
GilteritinibFLT3/AXL Inhibitor -
HY-19322B
PIM-447 dihydrochloridePIM Kinase Inhibitor -
HY-N1950
HispidulinPim-1 Inhibitor -
HY-N4149
QuercetagetinPim Inhibitor -
HY-16576A
SMI-4aPim-1 Inhibitor -
HY-15315
BaricitinibJAK1/2 Inhibitor -
HY-18086
TCS PIM-1 1Pim-1 Inhibitor -
HY-101947
SMI-16aPim Kinase Inhibitor -
HY-13001
QuizartinibFLT3 Inhibitor -
HY-101870B
Uzansertib phosphatePIM Inhibitor
Actividad biológica
Descripciòn
IC50 & Target
[1]|
PIM1 2 nM (Kd) |
PIM2 2 nM (Kd) |
PIM3 3 nM (Kd) |
FLT3-ITD |
In Vitro
In MOLM-13 and to a lesser extent in MV4-11 cells, a dose-dependent disruption of cell cycle with especially pronounced depletion of the S phase after treatment with SEL24-B489, accompanied by PARP cleavage and apoptosis was observed[1].
SEL24-B489 causes a profound inhibition of S6 (S235/236), but has little effect on PI3K/mTOR signaling[1].
SEL24-B489 inhibits STAT5 (Ser726) and reduced expression of MCL1, whereas none of the selective inhibitors altered c-MYC abundance or induced PARP cleavage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
-
Cell Line:AZD1208, AC220 and AraC in AML cell lines.
-
Concentration:0-10 μM.
-
Incubation Time:72 h.
-
Result:Decreased viability.
In Vivo
SEL24-B489 induces apoptosis of DLBCL cell lines in low/sub-micromolar concentrations and exhibits activity in a xenograft model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:SCID/beige mice bearing MV-4-11 tumors (FLT3-ITD+)[1].
-
Dosage:50, 75 and 100 mg/kg.
-
Administration:Orally, twice daily.
-
Result:Marked dose – dependent tumor reduction (67%, 74% and 82% tumor growth inhibition (TGI) for 50, 75 and 100 mg/kg daily doses, respectively).
Chemical Information
-
No. CAS 1616359-00-2
-
Appearance Solid
-
Peso molecular 446.14
-
Fòrmula C15H18Br2N4O2
-
Color Off-white to light yellow
-
SMILES
CC(N1C(C2CCNCC2)=NC3=C([N+]([O-])=O)C(Br)=C(Br)C=C31)C
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMF : 50 mg/mL (112.07 mM; Need ultrasonic)
DMSO : 25 mg/mL (56.04 mM; ultrasonic and adjust pH to 2 with HCl; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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% DMF 90% Corn Oil
Solubility: 5 mg/mL (11.21 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% 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 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 (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.
Pureza y Documentación
-
Ficha de datos (277 KB)
-
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
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 / DMF | 1 mM | 2.2414 mL | 11.2072 mL | 22.4145 mL | 56.0362 mL |
| 5 mM | 0.4483 mL | 2.2414 mL | 4.4829 mL | 11.2072 mL | |
| 10 mM | 0.2241 mL | 1.1207 mL | 2.2414 mL | 5.6036 mL | |
| 15 mM | 0.1494 mL | 0.7471 mL | 1.4943 mL | 3.7357 mL | |
| 20 mM | 0.1121 mL | 0.5604 mL | 1.1207 mL | 2.8018 mL | |
| 25 mM | 0.0897 mL | 0.4483 mL | 0.8966 mL | 2.2414 mL | |
| 30 mM | 0.0747 mL | 0.3736 mL | 0.7471 mL | 1.8679 mL | |
| 40 mM | 0.0560 mL | 0.2802 mL | 0.5604 mL | 1.4009 mL | |
| 50 mM | 0.0448 mL | 0.2241 mL | 0.4483 mL | 1.1207 mL | |
| DMF | 60 mM | 0.0374 mL | 0.1868 mL | 0.3736 mL | 0.9339 mL |
| 80 mM | 0.0280 mL | 0.1401 mL | 0.2802 mL | 0.7005 mL | |
| 100 mM | 0.0224 mL | 0.1121 mL | 0.2241 mL | 0.5604 mL |
SEL24-B489 Related Classifications
HY-120758 Related Classifications
Powered by Bioz