| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
ALK5 12 nM (IC50) ALK4 45 nM (IC50) ALK7 7.5 nM (IC50)
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|---|---|
| ln Vitro |
A83-01 sodium is a strong inhibitor of type I lymph node receptor ALK7, type I activin/lymph node receptor ALK4, and TGF-β type I receptor ALK5 kinase. It can lessen the amount of transcription that ALK-5 induces. ALK4-TD and ALK7-TD-induced transcription is also blocked by IC50 of Mv1Lu 12 nM in cells. The expression of constitutively active ALK-6, ALK-2, ALK-3, and ALK-1 induction is weakly inhibited by the IC50 in R4-2 cells, which is 45 nM and 7.5 nM, respectively. Effectively blocking the growth inhibitory impact of TGF-β, A 83-01 sodium (0.03-10 μM) totally suppresses this action at 3 μM. In HaCaT cells, TGF-β-induced Smad activation is inhibited by 83-01 sodium (1–10 μM) [1]. While TGF-β1 increases cell motility, adhesion, and invasion in HM-1 cells, 83-01 sodium (1 μM) does not alter cell proliferation [2].
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| ln Vivo |
Mice without body weight or neurobehavioral symptoms can have a considerably higher survival rate when administered with 83-01 (50, 150, and 500 μg/mouse) intraperitoneally [2]. In mice bearing M109 cells, 83-01 sodium (0.5 mg/kg, ip) sodium shows strong antitumor activity [3].
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| 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.
[2]. Yamamura S, et al. The activated transforming growth factor-beta signaling pathway in peritoneal metastases is a potential therapeutic target in ovarian cancer. Int J Cancer. 2012 Jan 1;130(1):20-8. [3]. Taniguchi Y, et al. Enhanced antitumor efficacy of folate-linked liposomal doxorubicin with TGF-β type I receptor inhibitor. Cancer Sci. 2010 Oct;101(10):2207-13 |
| Molecular Formula |
C25H19N5NAS
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|---|---|
| Molecular Weight |
444.51
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| CAS # |
2828431-89-4
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| Related CAS # |
A 83-01;909910-43-6;A 83-01;909910-43-6
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| SMILES |
C1C=C(C=CC=1)[N-]C(N1N=C(C(C2C3C(N=CC=2)=CC=CC=3)=C1)C1=CC=CC(C)=N1)=S.[Na+]
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (224.97 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (11.25 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2497 mL | 11.2483 mL | 22.4967 mL | |
| 5 mM | 0.4499 mL | 2.2497 mL | 4.4993 mL | |
| 10 mM | 0.2250 mL | 1.1248 mL | 2.2497 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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