Stenoparib | CAS#1140964-99-3 | PARP inhibitor

MedKoo Cat#: 205882 | Name: Stenoparib

Description:

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

Stenoparib, also known as E7449 and 2X-121, is an orally available small molecule inhibitor of the nuclear enzymes poly (ADP-ribose) polymerase (PARP) 1 and 2, with potential antineoplastic activity. Upon administration, E7449 selectively binds to PARP 1 and 2, thereby preventing the repair of damaged DNA via the base excision repair (BER) pathway. This agent enhances the accumulation of single and double strand DNA breaks and promotes genomic instability eventually leading to apoptosis. PARP 1/2 inhibitor E7449 may enhance the cytotoxicity of DNA-damaging agents and of radiotherapy. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins that signal and recruit other proteins to repair damaged DNA.

Chemical Structure

Stenoparib

CAS#1140964-99-3

Theoretical Analysis

MedKoo Cat#: 205882

Name: Stenoparib

CAS#: 1140964-99-3

Chemical Formula: C18H15N5O

Exact Mass: 317.1277

Molecular Weight: 317.34

Elemental Analysis: C, 68.13; H, 4.76; N, 22.07; O, 5.04

Price and Availability

Size	Price	Availability
25mg	USD 250.00	2 Weeks
50mg	USD 450.00	2 Weeks
100mg	USD 750.00	2 Weeks
200mg	USD 1,250.00	2 Weeks
500mg	USD 2,650.00	2 Weeks
1g	USD 3,850.00	2 Weeks
2g	USD 6,450.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

No Data

Synonym

E7449; E 7449; E-7449; 2X-121; 2X 121; 2X121; Stenoparib

IUPAC/Chemical Name

8-(isoindolin-2-ylmethyl)-2H-pyridazino[3,4,5-de]quinazolin-3(9H)-one

InChi Key

JLFSBHQQXIAQEC-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H15N5O/c24-18-13-6-3-7-14-16(13)17(21-22-18)20-15(19-14)10-23-8-11-4-1-2-5-12(11)9-23/h1-7H,8-10H2,(H,22,24)(H,19,20,21)

SMILES Code

O=C1NN=C(N2)C3=C(C=CC=C31)N=C2CN(C4)CC5=C4C=CC=C5

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, not in water

Shelf Life

>2 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

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#C9M07C22

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

E7449 is a PARP1 and PARP2 inhibitor and also inhibits TNKS1 and TNKS2, with IC50s of 2.0, 1.0, ∼50 and ∼50 nM for PARP1, PARP2, TNKS1 and TNKS2, respectively.

In vitro activity:

In wild type DT40 cells E7449 inhibited cell proliferation in a 2 day assay with an IC50 value of 3.2 μmol/L; this value was used for normalization of E7449 IC50 values obtained in mutant cells (Figure 1D, see Supplementary Figure 3 for representative IC50 curves). Reference: Oncotarget. 2015 Dec 1; 6(38): 41307–41323. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4747407/

In vivo activity:

In an in vivo subcutaneous MDA-MB-436 xenograft model, administration of E7449 at 30 or 100 mg/kg once daily for 28 days resulted in statistically significant antitumor activity (Figure 3B). A dose response was observed, with greater tumor growth inhibition at the higher 100 mg/kg dose. Reference: Oncotarget. 2015 Dec 1; 6(38): 41307–41323. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4747407/

	Solvent	mg/mL	mM
Solubility
	DMSO	0.2	0.63

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 317.34 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.

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. McGonigle S, Chen Z, Wu J, Chang P, Kolber-Simonds D, Ackermann K, Twine NC, Shie JL, Miu JT, Huang KC, Moniz GA, Nomoto K. E7449: A dual inhibitor of PARP1/2 and tankyrase1/2 inhibits growth of DNA repair deficient tumors and antagonizes Wnt signaling. Oncotarget. 2015 Dec 1;6(38):41307-23. doi: 10.18632/oncotarget.5846. PMID: 26513298; PMCID: PMC4747407.

In vitro protocol:

In vivo protocol:

1: Laurance J. Neurologists appeal to health secretary over withdrawal of drug for MS patients. BMJ. 2012 Nov 2;345:e7449. doi: 10.1136/bmj.e7449. PubMed PMID: 23125160. 2: Gilmore S, Hofmann-Wellenhof R, Muir J, Soyer HP. Lacunarity analysis: a promising method for the automated assessment of melanocytic naevi and melanoma. PLoS One. 2009 Oct 13;4(10):e7449. doi: 10.1371/journal.pone.0007449. PubMed PMID: 19823688; PubMed Central PMCID: PMC2758593.