Pyrido[2',3':4,5]pyrrolo[3,2-f]indazole, 7-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-1,9-dihydro-1-methyl-9-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]-
![Pyrido[2',3':4,5]pyrrolo[3,2-f]indazole, 7-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-1,9-dihydro-1-methyl-9-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]- Structure](CAS/20210111/GIF/2115742-03-3.gif)
- CAS No.
- 2115742-03-3
- Chemical Name:
- Pyrido[2',3':4,5]pyrrolo[3,2-f]indazole, 7-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-1,9-dihydro-1-methyl-9-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]-
- Synonyms
- NHWD-870;(S)-7-(1,4-Dimethyl-1H-1,2,3-triazol-5-yl)-1-methyl-9-(phenyl(tetrahydro-2H-pyran-4-yl)methyl)-1,9-dihydropyrido[2',3':4,5]pyrrolo[3,2-f]indazole;(S)-7-(1,4-Dimethyl-1H-1,2,3-triazol-5-yl)-1-methyl-9-(phenyl(tetrahydro-2H-pyran-4-yl)methyl)-1,9-dihydropyrido[2',3':4,5]pyrrolo[3,2-f]indazole;Pyrido[2',3':4,5]pyrrolo[3,2-f]indazole, 7-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-1,9-dihydro-1-methyl-9-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]-;NHWD 870,melanoma,cell-macrophage,bromodomains,Inhibitor,inhibit,oral,Epigenetic Reader Domain,selective,Apoptosis,NHWD-870,NHWD870,cancer,interaction
- CBNumber:
- CB38186622
- Molecular Formula:
- C29H29N7O
- Molecular Weight:
- 491.59
- MDL Number:
- MFCD33402167
- MOL File:
- 2115742-03-3.mol
Pyrido[2',3':4,5]pyrrolo[3,2-f]indazole, 7-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-1,9-dihydro-1-methyl-9-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]- Properties
| Boiling point | 687.3±65.0 °C(Predicted) |
|---|---|
| Density | 1.38±0.1 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility | DMSO : 125 mg/mL (254.28 mM; Need ultrasonic) |
| pka | 5.31±0.50(Predicted) |
| form | Solid |
| color | White to off-white |
Pyrido[2',3':4,5]pyrrolo[3,2-f]indazole, 7-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-1,9-dihydro-1-methyl-9-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]- price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0142664 | NHWD-870 | 2115742-03-3 | 5mg | $580 | 2021-12-16 | Buy |
| ChemScene | CS-0142664 | NHWD-870 | 2115742-03-3 | 10mg | $980 | 2021-12-16 | Buy |
| ChemScene | CS-0142664 | NHWD-870 | 2115742-03-3 | 25mg | $1900 | 2021-12-16 | Buy |
| ChemScene | CS-0142664 | NHWD-870 | 2115742-03-3 | 50mg | $3200 | 2021-12-16 | Buy |
| ChemScene | CS-0142664 | NHWD-870 | 2115742-03-3 | 100mg | $5000 | 2021-12-16 | Buy |
Pyrido[2',3':4,5]pyrrolo[3,2-f]indazole, 7-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-1,9-dihydro-1-methyl-9-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]- Chemical Properties,Uses,Production
Biological Activity
NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation[1]. NHWD-870 (0.01-10000 nM) inhibits melanoma cells (A375) with an IC50 of 2.46 nM[1].NHWD-870 (0-10000 nM; 5 dys) suppressed cell growth[1].NHWD-870 (0-50 nM; 24 hours) inhibits BRD4 phosphorylation and c-MYC expression[1].NHWD-870 exhibits mild inhibition of hERG channel (IC50 = 5.4 μM)[1].NHWD-870 shows robust activities inducing apoptosis and suppressing cell proliferation[1]. NHWD-870 (0.75-3 mg/kg; p.o.) has strong anti-tumor activities in mouse models[1].NHWD-870 reduces the number of tumor associated macrophages (TAMs) in subcutaneously implanted H526 and A2780 tumors. NHWD-870 downregulated CSF1 expression in tumor cells to inhibit TAM proliferation[1].NHWD-870 manifests diverse mechanisms of action in different cancer settings. These include: 1) inhibition of tumor cell growth by downregulating the PDGFRβ, MEK1/2 and STAT1/MYC signaling in tumor cells; 2) inhibition of tumor angiogenesis by decreasing PDGF production in tumor cells and the PDGFRβ and MEK1/2 signaling in endothelial cells. NHWD-870 has potent tumor suppressive efficacies in xenograft mouse models of small cell lung cancer, triple negative breast cancer and ovarian cancer[2].
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.
Pyrido[2',3':4,5]pyrrolo[3,2-f]indazole, 7-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-1,9-dihydro-1-methyl-9-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
Pyrido[2',3':4,5]pyrrolo[3,2-f]indazole, 7-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-1,9-dihydro-1-methyl-9-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| Changzhou PBpharmaceutical R&D Co.,Ltd | 0519-83990708 | lxy2046@yeah.net | China | 480 | 55 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24017 | 58 |
| Henan Alpha Chemical Co., Ltd. | 0371-55013243 15324716602 | 2853979810@qq.com | China | 10031 | 58 |
| https://hanhongsci.com/ | 021-54306202 18917919676 | info@hanhongsci.com | China | 29990 | 58 |
| Sichuan Yiyan Pharmaceutical Research | 19949968070 | 2904199885@qq.com | China | 918 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9155 | 58 |
| Nanjing Shizhou Biology Technology Co.,Ltd | 025-85560043 15850508050 | cindy.huang@synzest.com | China | 12007 | 58 |