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MedKoo Cat#: 462504 | Name: Senaparib free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Senaparib, also known as IMP4297, is s a novel highly potent and selective oral PARP1/2 inhibitor with strong antitumor activity in preclinical studies. Senaparib demonstrated encouraging clinical benefit and a favorable tolerability profile in patients with advanced solid tumour.

Chemical Structure

Senaparib free base
CAS#1401682-78-7 (free base)

Theoretical Analysis

MedKoo Cat#: 462504

Name: Senaparib free base

CAS#: 1401682-78-7 (free base)

Chemical Formula: C24H20F2N6O3

Exact Mass: 478.1565

Molecular Weight: 478.46

Elemental Analysis: C, 60.25; H, 4.21; F, 7.94; N, 17.57; O, 10.03

Price and Availability

Size Price Availability Quantity
5mg USD 110.00 Ready to ship
10mg USD 190.00 Ready to ship
25mg USD 350.00 Ready to ship
50mg USD 550.00 Ready to ship
100mg USD 950.00 Ready to ship
200mg USD 1,650.00 Ready to ship
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Related CAS #
1401683-39-3 (HCl) 1401682-78-7 (free base)
Synonym
Senaparib; IMP4297; IMP 4297; IMP-4297;
IUPAC/Chemical Name
5-fluoro-1-({4-fluoro-3-[4-(pyrimidin-2-yl)piperazine-1-carbonyl]phenyl}methyl)quinazoline-2,4(1H,3H)-dione
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)
SMILES Code
O=C(N1)N(CC2=CC=C(F)C(C(N3CCN(C4=NC=CC=N4)CC3)=O)=C2)C5=C(C(F)=CC=C5)C1=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
PARP inhibitors are promising anti-cancer agents with proven clinical activity based on mechanism of synthetic lethality.
Biological target:
Se-methylselenocysteine prevents tert-butyl hydroperoxide-induced increases in malondialdehyde (MDA) levels and glutathione reductase and glutathione peroxidase (GPX) activity, as well as decreases in glutathione (GSH) levels, in HepG2 cells. It also has an additive effect on irinotecan-induced tumor growth reduction in a FaDu mouse xenograft model.
In vitro activity:
To be determined
In vivo activity:
Senaparib is being investigated for its use in cancer treatment. In this first-in-human, phase 1, dose-escalation study, senarib was well tolerated in Australian patients with advanced solid tumors, with encouraging signals of antitumor activity. In 22 patients with evaluable disease, the overall response rate was 13.6%, and the disease control rate was 81.8%. The overall response rate was 33.3% for the BRCA mutation-positive subgroup and 6.3% for the nonmutated subgroup. Reference: Cancer. 2023 Apr 1;129(7):1041-1050. https://pubmed.ncbi.nlm.nih.gov/36718624/
Solvent mg/mL mM comments
Solubility
DMSO 83.3 174.17
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 478.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Cao J, Guo H, Ji D, Shen W, Zhang S, Hsieh CY, Xiong Cai S, Edward Tian Y, Xu C, Zhang P, Xu B. Safety, Tolerability, and Pharmacokinetics of Senaparib, a Novel PARP1/2 Inhibitor, in Chinese Patients With Advanced Solid Tumors: A Phase I Trial. Oncologist. 2023 Jun 20:oyad163. doi: 10.1093/oncolo/oyad163. Epub ahead of print. PMID: 37338150. 2. Gao B, Voskoboynik M, Cooper A, Wilkinson K, Hoon S, Hsieh CY, Cai S, Tian YE, Bao J, Ma N, Wang C, Zhang M, Li B, Guo M, Zhou R, Wang X, Xu C, de Souza P. A phase 1 dose-escalation study of the poly(ADP-ribose) polymerase inhibitor senaparib in Australian patients with advanced solid tumors. Cancer. 2023 Apr 1;129(7):1041-1050. doi: 10.1002/cncr.34662. Epub 2023 Jan 31. PMID: 36718624.
In vitro protocol:
To be determined
In vivo protocol:
1. Cao J, Guo H, Ji D, Shen W, Zhang S, Hsieh CY, Xiong Cai S, Edward Tian Y, Xu C, Zhang P, Xu B. Safety, Tolerability, and Pharmacokinetics of Senaparib, a Novel PARP1/2 Inhibitor, in Chinese Patients With Advanced Solid Tumors: A Phase I Trial. Oncologist. 2023 Jun 20:oyad163. doi: 10.1093/oncolo/oyad163. Epub ahead of print. PMID: 37338150. 2. Gao B, Voskoboynik M, Cooper A, Wilkinson K, Hoon S, Hsieh CY, Cai S, Tian YE, Bao J, Ma N, Wang C, Zhang M, Li B, Guo M, Zhou R, Wang X, Xu C, de Souza P. A phase 1 dose-escalation study of the poly(ADP-ribose) polymerase inhibitor senaparib in Australian patients with advanced solid tumors. Cancer. 2023 Apr 1;129(7):1041-1050. doi: 10.1002/cncr.34662. Epub 2023 Jan 31. PMID: 36718624.
1: Wu X, Liu J, Wang J, Wang L, Lin Z, Wang X, Zhu J, Kong B, Fei J, Tang Y, Xia B, Liang Z, Wang K, Huang Y, Zheng H, Lin A, Jiang K, Wang W, Wang X, Lou G, Pan H, Yao S, Li G, Hao M, Cai Y, Chen X, Yang Z, Chen Y, Wen H, Qu P, Xu C, Hsieh CY; FLAMES Investigators. Senaparib as first-line maintenance therapy in advanced ovarian cancer: a randomized phase 3 trial. Nat Med. 2024 Jun;30(6):1612-1621. doi: 10.1038/s41591-024-03003-9. Epub 2024 May 15. PMID: 38750351. 2: Cai SX, Ma N, Wang X, Guo M, Jiang Y, Tian YE. The Discovery of a Potent PARP1 Inhibitor Senaparib. Mol Cancer Ther. 2025 Jan 2;24(1):47-55. doi: 10.1158/1535-7163.MCT-23-0625. PMID: 38920409. 3: Meng X, Lin X, Jiang R, Lu Y, Zeng L, Cao M, Zhang J. Effect of Food on the Pharmacokinetics of Senaparib (IMP4297) in Healthy Chinese Subjects. Clin Drug Investig. 2022 Nov;42(11):1009-1016. doi: 10.1007/s40261-022-01198-8. Epub 2022 Oct 14. PMID: 36239914; PMCID: PMC9617823. 4: Gao B, Voskoboynik M, Cooper A, Wilkinson K, Hoon S, Hsieh CY, Cai S, Tian YE, Bao J, Ma N, Wang C, Zhang M, Li B, Guo M, Zhou R, Wang X, Xu C, de Souza P. A phase 1 dose-escalation study of the poly(ADP-ribose) polymerase inhibitor senaparib in Australian patients with advanced solid tumors. Cancer. 2023 Apr 1;129(7):1041-1050. doi: 10.1002/cncr.34662. Epub 2023 Jan 31. PMID: 36718624. 5: Hu X, Hsieh CY, Zhang Y, Liu W, Xu S, Cai SX, Liu L, Zhang M, Shi H, Zhang H, Liu P, Li X, Xu P. Effect of a strong CYP3A4 inhibitor and inducer on the pharmacokinetics of senaparib (IMP4297) in healthy volunteers: A drug-drug interaction study. Br J Clin Pharmacol. 2023 Jun;89(6):1767-1779. doi: 10.1111/bcp.15624. Epub 2023 Jan 3. PMID: 36458825. 6: Cao J, Guo H, Ji D, Shen W, Zhang S, Hsieh CY, Xiong Cai S, Edward Tian Y, Xu C, Zhang P, Xu B. Safety, Tolerability, and Pharmacokinetics of Senaparib, a Novel PARP1/2 Inhibitor, in Chinese Patients With Advanced Solid Tumors: A Phase I Trial. Oncologist. 2023 Dec 11;28(12):e1259-e1267. doi: 10.1093/oncolo/oyad163. PMID: 37338150; PMCID: PMC10712727.

View History

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