Art. -Nr.: HY-151289

ALK5-IN-34

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ALK5-IN-34 is an selective orally active activin receptor-like kinase (ALK) inhibitor. ALK5-IN-34 can inhibit the activity of ALK5-IN-34 with an IC₅₀ value of ≤10 nM. ALK5-IN-34 also has inhibitory of tumor growth and can be used for the research of proliferative diseases, such as cancer.

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Reinheit: 98.21%
CAS. Nr.: 2785430-90-0
Formel: C₂₃H₂₃N₇O
Molecular Weight:413.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ALK5-IN-34 Chemical Structure

CAS. Nr.: 2785430-90-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

ALK5

<10 nM (IC₅₀)

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen :

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen :

Smad1
Smad3

In Vitro

ALK5-IN-34 (EX-11) has kinase inhibition of ALK5 with an IC₅₀ value of ≤10 nM^[1].
ALK5-IN-34 has kinase selectivity of ALK2/ALK5 with an IC₅₀ value of ＜100 nM^[1].
ALK5-IN-34 shows TGFB-RI inhibition (RD-SMAD receptor activity) with an IC₅₀ value of ≤100 nM^[1].
ALK5-IN-34 (1 μM-10 nM) inhibits the expression of TGF-β-mediated alpha-SMA in a full concentration-dependent^[1].
ALK5-IN-34 (30, 300 and 3000 nM) suppresses the Treg frequency in a dose dependent manner^[1].
ALK5-IN-34 (0-0.1 μM; for 6 days or 7 days) inhibits FOXL2^CI34W-driven growth in KGN and COV434 cells with IC50 values of 140 nM and >10 μM, respectively^[1].
ALK5-IN-34 (10, 100 and 1000 nM; 2 h) shows a dose-dependent decrease in pSmad2 in KGN cell line^[1].
ALK5-IN-34 (30, 300 nM; 24 h) reverses the upregulation of gene expression in dose dependentent^[1].
ALK5-IN-34 (30, 300 nM; 24 h) increases HLA class I expression in dose-dependent^[1].

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

Cell Viability Assay^[1]

Cell Line:

KGN and COV434 cell lines
Concentration:

0-0.1 μM
Incubation Time:

for 6 days or 7 days
Result:

Inhibited FOXL2^CI34W-driven growth.

RT-PCR^[1]

Cell Line:

Human primary dermal fibroblasts
Concentration:

30, 300 nM
Incubation Time:

24 h
Result:

Reversed the upregulation of gene expression with TGFB stimulation.

In Vivo

ALK5-IN-34 (EX-11) (oral; 10-100 mg/kg) reduces the phopho SMAD2 levels (p-SMAD2) in a dose dependent manner in A549 murine xenograft model^[1].
ALK5-IN-34 (oral; 75 mg/kg; 0-24 h) shows reversely correlated between PK and tumor PD (pSMAD2 levels)^[1].
ALK5-IN-34 (oral; 150 mg/kg; bid; for 22 days) increases overall survival in ES-2 ovarian cancer mouse xenograft model and can delay progression^[1].
ALK5-IN-34 (p.o.; 75, 150 mg/kg; twice a day; for 21days) shows tumor growth inhibition (TGI) and increases the survival when combining with anti-PD-L1/anti-PD-1 in Syngeneic TNBC Model and in Subcutaneous Cloudman S91 melanoma model^[1].
ALK5-IN-34 (oral; 300, 1000 mg/kg; bid for 5 days) has good tolerability and safety margin in Tolerability Model^[1].

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

Animal Model:

A549 murine xenograft model^[1]
Dosage:

10, 50, 75 and 100 mg/kg
Administration:

oral gavage
Result:

Exhibited 92.5% inhibition based upon the average p-SMAD2 levels (75 mg/kg).

Animal Model:

EMT6 Syngeneic TNBC Model^[1]
Dosage:

75, 150 mg/kg
Administration:

p.o., twice a day, for 21days
Result:

Resulted significantly tumor growth inhibition (TGI) by 37% at 150 mg/kg.
Result in significant tumor growth inhibition (TGI) with combination of anti-PD-LI and resulted in a significant increase in mean survival by 37%.
Resulted in significant TGI by 34% with combination of anti-PD-1 and resulted in significant increase in mean survival by 26%.
Decreased the intra-tumoral pressure.

Animal Model:

Cachexia Model^[1]
Dosage:

150 mg/kg
Administration:

oral gavage, twice a day for 22 days
Result:

Showed reduction in total fluid volume and high whole limb weights.

Chemical Information

CAS. Nr. 2785430-90-0
Appearance Solid
Molecular Weight 413.48
Formel C₂₃H₂₃N₇O
Color Light yellow to green yellow
SMILES

CC1=CC=CC2=C(NC3=NC(NC4=CC=CC(N5CCOCC5)=C4)=NC=C3)C=NN=C12
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (241.85 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

2.4185 mL

12.0925 mL

24.1850 mL

5 mM

0.4837 mL

2.4185 mL

4.8370 mL

10 mM

0.2418 mL

1.2092 mL

2.4185 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. 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 (6.05 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 (6.05 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 (6.05 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 (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)
Handling Instructions (2659 KB)

Verweise

[1]. Bettina FRANZ, et al. Alk-5 inhibitors and uses thereof. Patent. WO2022126133A1.

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, 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	1 mM	2.4185 mL	12.0925 mL	24.1850 mL	60.4624 mL
	5 mM	0.4837 mL	2.4185 mL	4.8370 mL	12.0925 mL
	10 mM	0.2418 mL	1.2092 mL	2.4185 mL	6.0462 mL
	15 mM	0.1612 mL	0.8062 mL	1.6123 mL	4.0308 mL
	20 mM	0.1209 mL	0.6046 mL	1.2092 mL	3.0231 mL
	25 mM	0.0967 mL	0.4837 mL	0.9674 mL	2.4185 mL
	30 mM	0.0806 mL	0.4031 mL	0.8062 mL	2.0154 mL
	40 mM	0.0605 mL	0.3023 mL	0.6046 mL	1.5116 mL
	50 mM	0.0484 mL	0.2418 mL	0.4837 mL	1.2092 mL
	60 mM	0.0403 mL	0.2015 mL	0.4031 mL	1.0077 mL
	80 mM	0.0302 mL	0.1512 mL	0.3023 mL	0.7558 mL
	100 mM	0.0242 mL	0.1209 mL	0.2418 mL	0.6046 mL

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ALK5-IN-34

Kinase Inhibitor Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Wnt/Hedgehog/Notch Compound Library

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Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

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Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Fibrosis Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

ALK5-IN-34 Related Classifications

HY-151289 Related Classifications