| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
Melanoma cells (A375) are inhibited by NHWD-870 (0.01-10000 nM) at an IC50 of 2.46 nM[1]. 5 dys; NHWD-870, 0–10,000 nM) inhibited cell growth[1]. NHWD-870 (0–50 nM; 24 hours) suppresses the expression of c-MYC and BRD4 phosphorylation[1]. The hERG channel is mildly inhibited by NHWD-870 (IC50 = 5.4 µM)[1]. Strong effects on apoptosis induction and cell proliferation suppression are demonstrated by NHWD-870[1].
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| ln Vivo |
In mouse models, NHWD-870 (0.75-3 mg/kg; po) exhibits potent anti-tumor properties[1]. Tumor associated macrophages (TAMs) in subcutaneously implanted H526 and A2780 tumors are reduced by NHWD-870. reduced the expression of CSF1 in tumor cells to stop the growth of TAM[1]. distinct cancer situations result in distinct modes of action for NHWD-870. These include: 1) suppressing the proliferation of tumor cells by downregulating the signaling of PDGFRβ, MEK1/2, and STAT1/MYC in tumor cells; 2) suppressing the production of PDGF in tumor cells and the signaling of PDGFRβ and MEK1/2 in endothelial cells in tumor cells to prevent tumor angiogenesis. In xenograft mouse models of triple negative breast cancer, ovarian cancer, and small cell lung cancer, NHWD-870 has strong tumor suppression efficacies[2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: H526, A2780, ES-2, and MDA-MB231 cells Tested Concentrations: 0-10000 nM Incubation Duration: 5 days Experimental Results: demonstrated strong inhibitory activities against these cells in 5-day assays. Western Blot Analysis[1] Cell Types: H526, A2780, ES-2, and MDA-MB231 cells Tested Concentrations: 0- 50 nM Incubation Duration: 24 hrs (hours) Experimental Results: Led to the depletion of phosphorylated BRD4 and c-MYC at 10 nM. |
| Animal Protocol |
Animal/Disease Models: 4-6 weeks old female BALB/c nude mice/6-8 weeks old female C57BL/6 mice were used for B16F10 experiments (bearing NCI-H526, A2780, A375, B16F10, and TMD-8 cells)[1]
Doses: 0.75-3 mg/kg Route of Administration: Po; TMD8 and B16F10 melanoma model with one time/day for 11-21 days; A375 melanoma and PDX of melanoma with one time/day (5 days on, 2 days off) for 21 days. Experimental Results: Strongly suppressed the growth of established lung tumor, ovarian tumor, lymphoma, and melanoma in vivo. |
| References |
[1]. Yin M, et al. Potent BRD4 inhibitor suppresses cancer cell-macrophage interaction. Nat Commun. 2020;11(1):1833. Published 2020 Apr 14.
[2]. Nenghui Wang, et al. Abstract 1382: A novel BET family bromodomain inhibitor NHWD-870 represents a promising therapeutic agent for a broad spectrum of cancers. Molecular and Cellular Biology, Genetics. |
| Molecular Formula |
C29H29N7O
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|---|---|
| Molecular Weight |
491.59
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| CAS # |
2115742-03-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
C12N=CC(C3=C(C)N=NN3C)=CC=1N([C@@H](C1CCOCC1)C1=CC=CC=C1)C1C2=CC2C=NN(C)C=2C=1
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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) |
DMSO : 62.5 mg/mL (127.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.23 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 (4.23 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0342 mL | 10.1711 mL | 20.3422 mL | |
| 5 mM | 0.4068 mL | 2.0342 mL | 4.0684 mL | |
| 10 mM | 0.2034 mL | 1.0171 mL | 2.0342 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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