| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
BRM/BRG1 ATP Inhibitor-1 HCl, the hydrochloride salt of BRM/BRG1 ATP Inhibitor-1, is a novel,potent and orally bioactive inhibitor of Brahma Homolog (BRM)/SMARCA2 ATPase with the potential for the treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. It inhibits BRM/BRG1 ATP with an IC50 of 5 nM.
| ln Vitro |
Compound 14 (BRM/BRG1 ATP Inhibitor-1) (0–10 μM, 5 days) can stop cancer cells from proliferating [1]. The KRT80 gene expression is inhibited by BRM/BRG1 ATP Inhibitor-1, with an absolute AC50 (AAC50) value of 0.01 μM in H1299 cells and 0.01 μM in RERF-LC-AI cells [1].
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| ln Vivo |
Compound 14, also known as BRM/BRG1 ATP Inhibitor-1, can reduce KRT80 expression and tumor growth in a dose-dependent manner when taken orally for three weeks at a rate of 7.5 or 20 mg/kg [1].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: SKMEL5 melanoma cells and SBC-5 small cell carcinoma Tested Concentrations: 0-10 μM Incubation Duration: 5 days Experimental Results: Inhibited the proliferation of SKMEL5 cells with an AAC50 (absolute AC50) value of 0.004 μM and of SBC-5 cells with the AAC50more than 10 μM. |
| Animal Protocol |
Animal/Disease Models: Female athymic nude mice with RERF-LC-AI tumor xenografts[1]
Doses: 7.5 mg/kg, 20 mg/kg Route of Administration: Oral administration; everyday; 3 weeks Experimental Results: Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively. Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hrs (hours) after administration. |
| References |
| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.54 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 20.8 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. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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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