Senaparib (IMP4297) is a potent, selective, orally bioavailable PARP1/2 inhibitor. Senaparib (IMP4297) displays potent anti-tumor effects in animal models.

Physicochemical Properties

Molecular Formula	C24H20F2N6O3
Molecular Weight	478.450811386108
Exact Mass	478.16
Elemental Analysis	C, 60.25; H, 4.21; F, 7.94; N, 17.57; O, 10.03
CAS #	1401682-78-7
Related CAS #	1401682-78-7; 1401683-39-3 (HCl)
PubChem CID	68389008
Appearance	White to off-white solid powder
LogP	2
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	4
Heavy Atom Count	35
Complexity	804
Defined Atom Stereocenter Count	0
InChi Key	VBTUJTGLLREMNW-UHFFFAOYSA-N
InChi Code	InChI=1S/C24H20F2N6O3/c25-17-6-5-15(14-32-19-4-1-3-18(26)20(19)21(33)29-24(32)35)13-16(17)22(34)30-9-11-31(12-10-30)23-27-7-2-8-28-23/h1-8,13H,9-12,14H2,(H,29,33,35)
Chemical Name	5-fluoro-1-[[4-fluoro-3-(4-pyrimidin-2-ylpiperazine-1-carbonyl)phenyl]methyl]quinazoline-2,4-dione
Synonyms	IMP4297; IMP-4297; IMP 4297; Senaparib
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	Senaparib (IMP4297) is being studied as a therapy for pancreatic, breast, and advanced liver cancer [1].
References	[1]. 574P Updated results of phase I study of senaparib (IMP4297) in Australian patients with advanced solid tumours. ABSTRACT ONLY| VOLUME 31, SUPPLEMENT 4, S490, SEPTEMBER 01, 2020.
Additional Infomation	Senaparib is an orally bioavailable inhibitor of the nuclear enzymes poly (ADP-ribose) polymerase (PARP) 1 and 2, with potential antineoplastic activity. Upon administration, senaparib selectively binds to PARP 1 and 2 and prevents PARP-mediated DNA repair of single-strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks and promotes genomic instability and eventually leads to apoptosis. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA and is activated by single-strand DNA breaks. Drug Indication Treatment of metastatic castrate-resistant prostate cancer

Solubility Data

Solubility (In Vitro)

DMSO: ~83.3 mg/mL (~174.2 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2.08 mg/mL (4.35 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.0901 mL	10.4504 mL	20.9008 mL
	5 mM	0.4180 mL	2.0901 mL	4.1802 mL
	10 mM	0.2090 mL	1.0450 mL	2.0901 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.