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]- Struktur

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]-

Bezeichnung: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]-

CAS-Nr2115742-03-3

Englisch 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]-

CBNumberCB38186622

SummenformelC29H29N7O

Molgewicht491.59

MOL-Datei2115742-03-3.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]- physikalisch-chemischer Eigenschaften

Siedepunkt	687.3±65.0 °C(Predicted)
Dichte	1.38±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
Löslichkeit	DMSO : 125 mg/mL (254.28 mM; Need ultrasonic)
pka	5.31±0.50(Predicted)
Aggregatzustand	Solid
Farbe	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]- Chemische Eigenschaften,Einsatz,Produktion Methoden

Biologische Aktivität
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].
Einzelnachweise
[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]- Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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