4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one

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4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one Suppliers list
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4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one Basic information
Product Name:4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
Synonyms:4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one;1(2H)-Phthalazinone, 4-[[3-[[3-(5-bromo-2-furanyl)-5,6-dihydro-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]carbonyl]-4-fluorophenyl]methyl]-
CAS:3032451-66-1
MF:C25H18BrFN6O3
MW:549.35
EINECS:
Product Categories:
Mol File:3032451-66-1.mol
4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one Structure
4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one Chemical Properties
density 1.715±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
solubility DMSO: Soluble
pka12.059±0.40(predicted)
form Solid
color White to off-white
Safety Information
MSDS Information
4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one Usage And Synthesis
UsesYCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats[1].
in vivo

YCH1899 (5 mg/kg, intravenous injection ) has a moderate clearance rate in rats[1].
YCH1899 overcomes acquired Talazoparib resistance and has a significant regression of tumor volume in MDA-MB-436/OP (6.25, 12.5, and 25 mg/kg, orally, once a day for 27 days) and Capan-1/R-in vivo xenografts (12.5 and 25 mg/kg, orally, once a day for 21 days ) [1].

Animal Model:MDA-MB-436/OP xenografts and Capan-1/R-in vivo xenografts mice[1]
Dosage:12.5 and 25 mg/kg
Administration:Oral administration
Result:Inhibited MDA-MB-436/OP xenografts tumor growth with T/C of 36.74% and 15.29% at 12.5 and 25 mg/kg
Inhibited Capan-1/R xenografts tumor growth with T/C of 48.92% and 13.87% at 12.5 and 25 mg/kg.
Animal Model:rats[1]
Dosage:5 mg/kg
Administration:Intravenous injection
Result:Had a moderate clearance rate (24.5 mL/min/kg) and half-life (3.25 h).
IC 50PARP-1: <0.001 nM (IC50); PARP-2: <0.001 nM (IC50); PARP3: 1.1 nM (IC50); PARP4: 1.0 nM (IC50); TNKS1: 3.8 nM (EC50); TNKS2: 12.4 nM (IC50); PARA6: 9.5 nM (IC50); PARP-7: 7.3 nM (IC50); ARTD10/PARP10: 10.8 nM (IC50); PARA11: 2.166 μM (IC50); human PARP12: 14.1 nM (IC50); PARP14: 35.914 μM (IC50); PARP15: 51.623 nM (IC50)
References[1] Sun Y, et al. YCH1899, a Highly Effective Phthalazin-1(2H)-one Derivative That Overcomes Resistance to Prior PARP Inhibitors. J Med Chem. 2023 Aug 21. DOI:10.1021/acs.jmedchem.3c00821
4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one Preparation Products And Raw materials
Tag:4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one(3032451-66-1) Related Product Information
4-(3-(3-(5-bromofuran-2-yl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine-7-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one Rucaparib Camsylate Rucaparib AZD2461 3-Pyridinecarbonitrile, 6-[4-[(1,2,3,4,5,6-hexahydro-5-oxobenzo[h]-1,6-naphthyridin-8-yl)methyl]-1-piperazinyl]- PF-01367338