Art. -Nr.: HY-155195

FLT3/CHK1-IN-1

Name: FLT3/CHK1-IN-1
Brand: MedChemExpress
SKU: HY-155195
Price: 461.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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FLT3/CHK-IN-1 (Compound 18) is a dual inhibitor of FLT3/CHK1. FLT3/CHK-IN-1 is more than 1700 times more selective to c-KI T and greatly reduces hERG affinity with an IC₅₀ value of 58.4 μM. FLT3/CHK-IN-1 inhibits tumor growth in mouse xenotransplantation models inoculated with MV-4-11 cells.

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Reinheit : 99.37%
CAS. Nr.: 2991054-23-8
Formel: C₂₅H₃₃F₃N₆O₂
Molecular Weight:506.56

Speicherung:

4°C, protect from light

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

FLT3/CHK1-IN-1 Chemical Structure

CAS. Nr.: 2991054-23-8

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Biologische Aktivität
- Beschreibung
- Cellular Effect
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	8.2 nM Compound: 18	Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-N701K mutation assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against mouse BaF3 cells harboring FLT3-ITD-N701K mutation assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 37584545]
JeKo-1	IC₅₀	260 nM Compound: 18	Antiproliferative activity against human JeKo-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human JeKo-1 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 37584545]
MV4-11	IC₅₀	0.21 nM Compound: 18	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 37584545]
Z-138	IC₅₀	115 nM Compound: 18	Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay Antiproliferative activity against human Z138 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter 96 Aqueous One Solution Cell Proliferation Assay	[PMID: 37584545]

Chemical Information

CAS. Nr. 2991054-23-8
Appearance Solid
Molecular Weight 506.56
Formel C₂₅H₃₃F₃N₆O₂
Color White to off-white
SMILES

N[C@H]1CC[C@@H](NC2=NC(NC3=CC4=C(C=C3)CN(C(CC(O)(C)C)=O)CC4)=NC=C2C(F)(F)F)CC1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (197.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9741 mL

9.8705 mL

19.7410 mL

5 mM

0.3948 mL

1.9741 mL

3.9482 mL

10 mM

0.1974 mL

0.9870 mL

1.9741 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (4.94 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.94 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (4.94 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Li X, et al. Discovery of 2-Aminopyrimidine Derivatives as Potent Dual FLT3/CHK1 Inhibitors with Significantly Reduced hERG Inhibitory Activities. J Med Chem. 2023 Sep 14;66(17):11792-11814. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9741 mL	9.8705 mL	19.7410 mL	49.3525 mL
	5 mM	0.3948 mL	1.9741 mL	3.9482 mL	9.8705 mL
	10 mM	0.1974 mL	0.9870 mL	1.9741 mL	4.9352 mL
	15 mM	0.1316 mL	0.6580 mL	1.3161 mL	3.2902 mL
	20 mM	0.0987 mL	0.4935 mL	0.9870 mL	2.4676 mL
	25 mM	0.0790 mL	0.3948 mL	0.7896 mL	1.9741 mL
	30 mM	0.0658 mL	0.3290 mL	0.6580 mL	1.6451 mL
	40 mM	0.0494 mL	0.2468 mL	0.4935 mL	1.2338 mL
	50 mM	0.0395 mL	0.1974 mL	0.3948 mL	0.9870 mL
	60 mM	0.0329 mL	0.1645 mL	0.3290 mL	0.8225 mL
	80 mM	0.0247 mL	0.1234 mL	0.2468 mL	0.6169 mL
	100 mM	0.0197 mL	0.0987 mL	0.1974 mL	0.4935 mL

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FLT3/CHK1-IN-1