A 77-01 | TGF-β Receptor Inhibitor - MedChemExpress

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                                1. TGF-beta/Smad
                                2. TGF-β Receptor
                                3. A 77-01
                                A 77-01 Cat. No.: HY-78349 Purity: 99.92% FAQs Data Sheet SDS COA Handling Instructions

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                                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

                                Size Price Stock Quantity
                                Free Sample (0.1 - 0.5 mg) Apply Now
                                Solid + Solvent (Highly Recommended)
                                10 mM * 1 mL in DMSO ready for reconstitution USD 129 In-stock 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31
                                Solution
                                10 mM * 1 mL in DMSO USD 129 In-stock 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31
                                Solid
                                5 mg USD 118 In-stock 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31
                                10 mg USD 176 In-stock 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31
                                25 mg USD 317 In-stock 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31
                                50 mg USD 460 In-stock 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31
                                100 mg USD 645 In-stock 0 1 2 3 4 5 6 7 Estimated Time of Arrival: December 31
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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

                                • Mol Med Rep. 2018 May;17(5):6301-6310. [Abstract]
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                                Related Small Molecules:

                                Related Proteins:

                                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.

                                607737-87-1

                                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
                                10 mM 0.3492 mL 1.7462 mL 3.4925 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 kg g mg μg ng pg = Concentration M mM μM nM pM × Volume L mL μL × Molecular Weight *

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

                                This equation is commonly abbreviated as: C1V1 = C2V2

                                Concentration (start) M mM μM nM pM

                                C1

                                × Volume (start) L mL μL

                                V1

                                = Concentration (final) M mM μM nM pM

                                C2

                                × Volume (final) L mL μL

                                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.
                                • Protocol 3

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

                                  Solubility: ≥ 2.5 mg/mL (8.73 mM); Clear solution

                                  This protocol yields a clear solution of ≥ 2.5 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 (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

                                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). Tel: 609-228-6898 E-mail: [email protected] Technical Support: [email protected] 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. Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution 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%

                                Select Batch: HY-78349-606608 HY-78349-09313 HY-78349-307521 Data Sheet (280 KB) SDS (393 KB)

                                COA (255 KB) LCMS (95 KB)

                                Handling Instructions (2659 KB)
                                References
                                • [1]. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800. [Content Brief]

                                • [1]. Tojo M, et al. The ALK-5 inhibitor A-83-01 inhibits Smad signaling and epithelial-to-mesenchymal transition by transforming growth factor-beta. Cancer Sci. 2005 Nov;96(11):791-800.

                                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

                                • Cancer
                                • Cancer Targeted Therapy Cancer Immunotherapy Cancer Metabolism and Metastasis
                                • TGF-beta/Smad
                                • TGF-β Receptor
                                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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