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]- manufacturers
- NHWD-870
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- $1630.00
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2026-05-11
- CAS:2115742-03-3
- Purity:
- Supply Ability: 10g
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| | 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]- Basic information |
| Product 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: | 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;(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;NHWD-870 | | CAS: | 2115742-03-3 | | MF: | C29H29N7O | | MW: | 491.59 | | EINECS: | | | Product Categories: | | | 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]- Structure](CAS/20210111/GIF/2115742-03-3.gif) |
| | 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 |
| 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]- Usage And Synthesis |
| Uses | 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]. | | 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]. | | in vivo | 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]. | Animal Model: | 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] | | Dosage: | 0.75-3 mg/kg | | Administration: | P.o.; TMD8 and B16F10 melanoma model with once daily for 11-21 days; A375 melanoma and PDX of melanoma with once daily (5 days on, 2 days off) for 21 days. | | Result: | Strongly suppressed the growth of established lung tumor, ovarian tumor, lymphoma, and melanoma in vivo.
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| | 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 |
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