Art. -Nr.: HY-124944

APS6-45

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APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.

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Reinheit: 99.51%
CAS. Nr.: 2188236-41-9
Formel: C₂₃H₁₆F₈N₄O₃
Molecular Weight:548.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

APS6-45 Chemical Structure

CAS. Nr.: 2188236-41-9

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

Biologische Aktivität

Beschreibung

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity^[1].

Alle Ras Isoform-spezifische Produkte anzeigen :

In Vitro

APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay^[1].
APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1^[1].

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

In Vivo

APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight^[1].
APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice^[1].
APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), C_max (9.7 µM) and AUC_0-24 (123.7 µM•h) in mice^[1].

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

Animal Model:

Female nude mice (6 weeks) are implanted with TT cells^[1]
Dosage:

10 mg/kg
Administration:

P.o. daily for 30 days
Result:

Led to partial or complete responses in 75% and was well tolerated.

Animal Model:

Male ICR mice (6 weeks of age)^[1]
Dosage:

20 mg/kg (Pharmacokinetic Analysis)
Administration:

A single p.o.
Result:

T_1/2=5.6 h, C_max=9.7 µM, AUC_0-24=123.7 µM•h.

Chemical Information

CAS. Nr. 2188236-41-9
Appearance Solid
Molecular Weight 548.39
Formel C₂₃H₁₆F₈N₄O₃
Color Off-white to light yellow
SMILES

O=C(C1=NC=CC(OC2=CC=C(C=C2)NC(NC3=CC(C(F)(C(F)(F)F)C(F)(F)F)=CC=C3F)=O)=C1)NC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 250 mg/mL (455.88 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

1.8235 mL

9.1176 mL

18.2352 mL

5 mM

0.3647 mL

1.8235 mL

3.6470 mL

10 mM

0.1824 mL

0.9118 mL

1.8235 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.79 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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)
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]. Sonoshita M, et, al. A whole-animal platform to advance a clinical kinase inhibitor into new disease space. Nat Chem Biol. 2018 Mar;14(3):291-298. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8235 mL	9.1176 mL	18.2352 mL	45.5880 mL
	5 mM	0.3647 mL	1.8235 mL	3.6470 mL	9.1176 mL
	10 mM	0.1824 mL	0.9118 mL	1.8235 mL	4.5588 mL
	15 mM	0.1216 mL	0.6078 mL	1.2157 mL	3.0392 mL
	20 mM	0.0912 mL	0.4559 mL	0.9118 mL	2.2794 mL
	25 mM	0.0729 mL	0.3647 mL	0.7294 mL	1.8235 mL
	30 mM	0.0608 mL	0.3039 mL	0.6078 mL	1.5196 mL
	40 mM	0.0456 mL	0.2279 mL	0.4559 mL	1.1397 mL
	50 mM	0.0365 mL	0.1824 mL	0.3647 mL	0.9118 mL
	60 mM	0.0304 mL	0.1520 mL	0.3039 mL	0.7598 mL
	80 mM	0.0228 mL	0.1140 mL	0.2279 mL	0.5698 mL
	100 mM	0.0182 mL	0.0912 mL	0.1824 mL	0.4559 mL

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APS6-45

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Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

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Ferroptosis Compound Library

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Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

APS6-45

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Alle Ras Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

APS6-45 Related Classifications

HY-124944 Related Classifications