SB-505124 hydrochloride

Name: SB-505124 hydrochloride
Brand: MedChemExpress
SKU: HY-13521A
Rating: 5.0 (20 reviews)

Cat. No.: HY-13521A Purity: 99.34%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

SB-505124 hydrochloride is a selective inhibitor of?TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with?IC₅₀s?of 129 nM and 47 nM for?ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.

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

SB-505124 hydrochloride Chemical Structure

CAS No. : 356559-13-2

Size	Price	Stock	Quantity
5 mg	USD 101	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 158	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 475	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 20 publication(s) in Google Scholar

Other Forms of SB-505124 hydrochloride:

SB-505124 In-stock

17 Publications Citing Use of MCE SB-505124 hydrochloride

: SB-505124 hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075. [Abstract]; Treatment with SB505124 for 3 days significantly increases apoptosis at 4 and 8 μM in WERI Rb1.

: SB-505124 hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075. [Abstract]; Treatment with SB505124 for 3 days significantly increases apoptosis at 4 and 8 μM in WERI Rb1.

: SB-505124 hydrochloride purchased from MedChemExpress. Usage Cited in: Oncogene. 2019 Mar;38(12):2056-2075. [Abstract]; The effects on growth and invasion are paralleled by a dose-dependent inhibition in SMAD2 phosphorylation upon treatment with SB505124 at 0.5, 1, 2, 3, 4, 8 μM for 4 days.

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 129 nM (ALK4), 47 nM (ALK5)

In Vitro

SB-505124 demonstrates no toxicity to renal epithelial A498 cells at concentrations up to 100 μM for 48 h. 505124 inhibits the closely related ALK4 with an IC₅₀ value of 129±11 nM (about 2.5-fold less sensitive than ALK5) but does not inhibit ALK2 at concentrations up to 10 μM. SB-505124 (1 μM) inhibits the TGF-β-induced phosphorylation of Smad2 in all three of these cell lines in a concentration-dependent fashion. SB-505124 (1 or 5 μM) potently inhibits TGF-β-induced activation of JNK/SAP, extracellular signal-regulated kinase 1/2, and p38 despite the different patterns of activation in these cells^[1]. SB-505124 (10 μM) impairs Smad2 phosphorylation and CTGF and α-SMA expression in vitro^[2]. SB-505124 susspresses CTGF and α-SMA observed by immunofluorescence. Cell outgrowth from explants dissected from eyes to which SB-505124 is applied during GFS is robust while outgrowth is poor from those treated with MMC^[3].

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

In Vivo

SB-505124 (5 mg/kg; i.p.) alone has no effect in C57Bl6 mice with A549 xenografts, but administration of SB-505124 with a single dose of Carboplatin (60 mg/kg) results in durable responses without the need for maintenance therapy in five animals^[4].

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

Animal Model:	C57Bl6 mice with A549 xenografts^[4]
Dosage:	5 mg/kg
Administration:	I.p.; daily
Result:	Had no effect alone, but administration with a single dose of carboplatin (60 mg/kg) resulted in durable responses without the need for maintenance therapy in five animals.

Molecular Weight

371.86

Formula

C₂₀H₂₂ClN₃O₂

CAS No.

356559-13-2

Appearance

Solid

Color

Light yellow to green yellow

SMILES

CC1=CC=CC(C2=C(C3=CC=C(OCO4)C4=C3)N=C(C(C)(C)C)N2)=N1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

Methanol : 125 mg/mL (336.15 mM; Need ultrasonic)

DMSO : 50 mg/mL (134.46 mM; ultrasonic and warming and heat to 60°C; 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	2.6892 mL	13.4459 mL	26.8918 mL
5 mM	0.5378 mL	2.6892 mL	5.3784 mL
10 mM	0.2689 mL	1.3446 mL	2.6892 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (6.72 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 (6.72 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)

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.34%

Select Batch:

Data Sheet (282 KB) SDS (252 KB)

COA (258 KB) HNMR (254 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. DaCosta Byfield S, et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. Mol Pharmacol. 2004 Mar;65(3):744-52. [Content Brief]

[2]. Sutariya V, et al. Thermoreversible gel for delivery of receptor-like kinase 5 inhibitor SB-505124 for glaucoma filtration surgery. Pharm Dev Technol. 2013 Jul-Aug;18(4):957-62. [Content Brief]

[3]. Sapitro J, et al. Suppression of transforming growth factor-β effects in rabbit subconjunctival fibroblasts by receptor-like kinase 5 inhibitor. Mol Vis. 2010 Sep 16;16:1880-92. [Content Brief]

[4]. Marini KD, et al. Inhibition of activin signaling in lung adenocarcinoma increases the therapeutic index of platinum chemotherapy. Sci Transl Med. 2018 Jul 25;10(451). pii: eaat3504. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / Methanol	1 mM	2.6892 mL	13.4459 mL	26.8918 mL	67.2296 mL
	5 mM	0.5378 mL	2.6892 mL	5.3784 mL	13.4459 mL
	10 mM	0.2689 mL	1.3446 mL	2.6892 mL	6.7230 mL
	15 mM	0.1793 mL	0.8964 mL	1.7928 mL	4.4820 mL
	20 mM	0.1345 mL	0.6723 mL	1.3446 mL	3.3615 mL
	25 mM	0.1076 mL	0.5378 mL	1.0757 mL	2.6892 mL
	30 mM	0.0896 mL	0.4482 mL	0.8964 mL	2.2410 mL
	40 mM	0.0672 mL	0.3361 mL	0.6723 mL	1.6807 mL
	50 mM	0.0538 mL	0.2689 mL	0.5378 mL	1.3446 mL
	60 mM	0.0448 mL	0.2241 mL	0.4482 mL	1.1205 mL
	80 mM	0.0336 mL	0.1681 mL	0.3361 mL	0.8404 mL
	100 mM	0.0269 mL	0.1345 mL	0.2689 mL	0.6723 mL