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
- CAS No.
- 3032451-66-1
- Chemical 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]-
- CBNumber:
- CB414980392
- Molecular Formula:
- C25H18BrFN6O3
- Molecular Weight:
- 549.35
- MDL Number:
- MOL File:
- 3032451-66-1.mol
- MSDS File:
- SDS
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 price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 39737 | YCH1899 ≥98% | 3032451-66-1 | 1mg | $54 | 2026-04-30 | Buy |
| Cayman Chemical | 39737 | YCH1899 ≥98% | 3032451-66-1 | 5mg | $257 | 2026-04-30 | Buy |
| Cayman Chemical | 39737 | YCH1899 ≥98% | 3032451-66-1 | 10mg | $486 | 2026-04-30 | Buy |
| ChemScene | CS-0890941 | YCH1899 99.39% | 3032451-66-1 | 5mg | $217 | 2026-06-04 | Buy |
| ChemScene | CS-0890941 | YCH1899 99.39% | 3032451-66-1 | 10mg | $352 | 2026-06-04 | Buy |
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,Uses,Production
Uses
YCH1899 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 50
PARP-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
Raw materials
Preparation Products
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
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Beckham Medical Technology Co., Ltd | 13816613772 | huahero21@sina.com | China | 2996 | 55 |
| Guangzhou Younan Technology Co., Ltd | 020-82000279 18988941452 | YN_research@163.com | China | 2984 | 58 |
| AnEasyTech Shanghai Co., Ltd. | 13916181326 | info@aneasytech.com | China | 192 | 58 |
| Supplier | Advantage |
|---|---|
| Shanghai Beckham Medical Technology Co., Ltd | 55 |
| Guangzhou Younan Technology Co., Ltd | 58 |
| AnEasyTech Shanghai Co., Ltd. | 58 |




