2. TGF-beta/Smad
  3. TGF-β Receptor
  4. A 77-01

A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.

For research use only. We do not sell to patients.

A 77-01 Chemical Structure

A 77-01 Chemical Structure

CAS No. : 607737-87-1

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

A 77-01 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE A 77-01

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms
ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM[1].

IC50 & Target

IC50: 25 nM (ALK5)[1]
In Vitro

A-77-01 (0.01-10 µM; 25 hours; Mv1Lu cells) treatment effectively inhibits TGF-β-induced transcriptional activation in concentration-dependent fashion[1].
A-77-01 (1 µM; 24-72 hours; Mv1Lu cells) treatment efficiently prevents the growth-inhibitory effects of TGF-β[1].
A-77-01 (1 µM; 30 minutes; HaCaT cells) treatment inhibits TGF-β-induced phosphorylation of Smad2[1].

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

A 77-01 Related Antibodies

RT-PCR[1]

Cell Line: Mv1Lu cells
Concentration: 0.01 µM, 0.03 µM, 0.1 µM, 0.3 µM, 1 µM, 3 µM, 10 µM
Incubation Time: 25 hours
Result: Inhibited the luciferase activity induced by TGF-β in concentration-dependent fashion.

Cell Viability Assay[1]

Cell Line: Mv1Lu cells
Concentration: 1 µM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Efficiently prevented the growth-inhibitory effects of TGF-β.

Western Blot Analysis[1]

Cell Line: HaCaT cells
Concentration: 1 µM
Incubation Time: 30 minutes
Result: Inhibited TGF-β-induced phosphorylation of Smad2.
Molecular Weight

286.33

Formula

C18H14N4
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=CC=CC(C2=NNC=C2C3=CC=NC4=CC=CC=C34)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (87.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4925 mL 17.4624 mL 34.9247 mL
5 mM 0.6985 mL 3.4925 mL 6.9849 mL
View the 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (8.73 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (8.73 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.92%

SDS (393 KB)

COA (255 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

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, 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 3.4925 mL 17.4624 mL 34.9247 mL 87.3118 mL
5 mM 0.6985 mL 3.4925 mL 6.9849 mL 17.4624 mL
10 mM 0.3492 mL 1.7462 mL 3.4925 mL 8.7312 mL
15 mM 0.2328 mL 1.1642 mL 2.3283 mL 5.8208 mL
20 mM 0.1746 mL 0.8731 mL 1.7462 mL 4.3656 mL
25 mM 0.1397 mL 0.6985 mL 1.3970 mL 3.4925 mL
30 mM 0.1164 mL 0.5821 mL 1.1642 mL 2.9104 mL
40 mM 0.0873 mL 0.4366 mL 0.8731 mL 2.1828 mL
50 mM 0.0698 mL 0.3492 mL 0.6985 mL 1.7462 mL
60 mM 0.0582 mL 0.2910 mL 0.5821 mL 1.4552 mL
80 mM 0.0437 mL 0.2183 mL 0.4366 mL 1.0914 mL
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A 77-01 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

A 77-01607737-87-1TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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