Cat. No.: HY-18507

AD57

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AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity.

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Pureté: 98.27%
CAS No.: 1093380-42-7
Formule: C₂₂H₂₀F₃N₇O
Masse moléculaire:455.44

Stockage:

4°C, protect from light

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

AD57 Chemical Structure

CAS No.: 1093380-42-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity^[1].

IC₅₀ & Target^[1]

Braf

Voir tous les produits spécifiques à Isoform Raf :

Voir tous les produits spécifiques à Isoform Ribosomal S6 Kinase (RSK) :

Voir tous les produits spécifiques à Isoform Src :

In Vitro

AD57 (0.2 nM) significantly inhibits the ptc > dRet^MEN2B lethality in the larva of Drosophila^[1].
AD57 (0.1 nM) enhances survival of ptc > dRet^MEN2B by reducing erk gene dosage in Drosophila^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AD57 inhibits the viability of MEN2B (MZ-CRC-1) and MEN2A (TT) patient-derived cell lines in RET^MEN2 models^[1].
AD57 (20 mg/kg) significantly inhibits TT-based tumour growth without obvious cytotoxicity in conventional mouse xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 1093380-42-7
Appearance Solid
Masse moléculaire 455.44
Formule C₂₂H₂₀F₃N₇O
Color Off-white to light yellow
SMILES

O=C(NC1=CC=CC(C(F)(F)F)=C1)NC2=CC=C(C3=NN(C(C)C)C4=C3C(N)=NC=N4)C=C2
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light

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

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (274.46 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

2.1957 mL

10.9784 mL

21.9568 mL

5 mM

0.4391 mL

2.1957 mL

4.3914 mL

10 mM

0.2196 mL

1.0978 mL

2.1957 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.08 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). 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 (20.8 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 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)
Instruction de manipulation (2659 KB)

Références

[1]. Dar AC, et al. Chemical genetic discovery of targets and anti-targets for cancer polypharmacology. Nature. 2012 Jun 6;486(7401):80-4. [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	2.1957 mL	10.9784 mL	21.9568 mL	54.8920 mL
	5 mM	0.4391 mL	2.1957 mL	4.3914 mL	10.9784 mL
	10 mM	0.2196 mL	1.0978 mL	2.1957 mL	5.4892 mL
	15 mM	0.1464 mL	0.7319 mL	1.4638 mL	3.6595 mL
	20 mM	0.1098 mL	0.5489 mL	1.0978 mL	2.7446 mL
	25 mM	0.0878 mL	0.4391 mL	0.8783 mL	2.1957 mL
	30 mM	0.0732 mL	0.3659 mL	0.7319 mL	1.8297 mL
	40 mM	0.0549 mL	0.2745 mL	0.5489 mL	1.3723 mL
	50 mM	0.0439 mL	0.2196 mL	0.4391 mL	1.0978 mL
	60 mM	0.0366 mL	0.1830 mL	0.3659 mL	0.9149 mL
	80 mM	0.0274 mL	0.1372 mL	0.2745 mL	0.6861 mL
	100 mM	0.0220 mL	0.1098 mL	0.2196 mL	0.5489 mL

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Voir tous les produits spécifiques à Isoform Raf

Voir tous les produits spécifiques à Isoform Ribosomal S6 Kinase (RSK)

Voir tous les produits spécifiques à Isoform Src

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

AD57 Related Classifications

HY-18507 Related Classifications