WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206119
CAS#: 922139-31-9 (sodium)
Description: Recilisib, also known as ON 01210.Na, is a radioprotectant, which modifys cell cycle distribution patterns in cancer cells subjected to radiation therapy, and it has been identified as a potential candidate for radiation protection studies. It appears that Recilisib radioprotective mechanisms involve prevention of p53-dependent and independent radiation-induced apoptosis.
Hodoodo Cat#: H206119
Name: Recilisib sodium
CAS#: 922139-31-9 (sodium)
Chemical Formula: C16H12ClNaO4S
Exact Mass: 0.00
Molecular Weight: 358.770
Elemental Analysis: C, 53.57; H, 3.37; Cl, 9.88; Na, 6.41; O, 17.84; S, 8.94
Related CAS #: 334969-03-8 (free base) 922139-31-9 (sodium)
Synonym: Recilisib sodium; ON 01210.Na; ON-01210; ON01210; ON01210; Brand name: Ex-RAD
IUPAC/Chemical Name: sodium (E)-4-(2-((4-chlorobenzyl)sulfonyl)vinyl)benzoate
InChi Key: PRFBWBYKWZVQJF-RRABGKBLSA-M
InChi Code: InChI=1S/C16H13ClO4S.Na/c17-15-7-3-13(4-8-15)11-22(20,21)10-9-12-1-5-14(6-2-12)16(18)19;/h1-10H,11H2,(H,18,19);/q;+1/p-1/b10-9+;
SMILES Code: O=C([O-])C1=CC=C(/C=C/S(=O)(CC2=CC=C(Cl)C=C2)=O)C=C1.[Na+]
Appearance: white 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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
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: Related CAS# CAS#334969-03-8 (Recilisib free) CAS#922139-31-9 (Recilisib sodium)
| Biological target: | TBD |
| In vitro activity: | In this report ON01210.Na provides significant dose dependent radiation protection both In Vitro and In Vivo (Figure 1, Figure 5) by protecting the hematopoietic system. ON01210.Na, unlike many of the other compounds in this library, was non-toxic to normal cells derived from human fetal lung fibroblasts (HFL cells), HUVECs (Figure 2) and to normal human bone marrow cells (Figure 4). ON01210.Na has the chemical characteristics necessary for large-scale production and long-term stability necessary for administration to a large number of first responders (data not shown). This compound was also found to be water soluble and orally bio-available with very favorable pharmacokinetic properties in multiple routes of administration (data not shown). Reference: PLoS One. 2013; 8(3): e58355. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3591351/ |
| In vivo activity: | Mice that received Ex-RAD (Recilisib) doses of 500 mg/kg exhibited a significant increase in survival as compared with either vehicle control group or the lowest dose of Ex-RAD, 25 mg/kg treated group (P < 0.0033, Fisher's exact test). No apparent toxicity was observed with the highest dose (500 mg/kg) used in this study. Surviving animals were healthy at the end of the study (30 day after radiation). The optimal 500 mg/kg dose was used to obtain the DRF for Ex-RAD. The drug was administered to mice 24 h and 15 min (two doses) before TBI at various radiation doses, and survival data were used to evaluate the DRF. Reference: J Radiat Res. 2012 Jul; 53(4): 526–536. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3393340/ |
The following data is based on the product molecular weight 358.77 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. Kang AD, Cosenza SC, Bonagura M, Manair M, Reddy MV, Reddy EP. ON01210.Na (Ex-RAD®) mitigates radiation damage through activation of the AKT pathway. PLoS One. 2013;8(3):e58355. doi: 10.1371/journal.pone.0058355. Epub 2013 Mar 7. PMID: 23505494; PMCID: PMC3591351. 2. Li Y, Girgis M, Wise SY, Fatanmi OO, Seed TM, Maniar M, Cheema AK, Singh VK. Analysis of the metabolomic profile in serum of irradiated nonhuman primates treated with Ex-Rad, a radiation countermeasure. Sci Rep. 2021 Jun 1;11(1):11449. doi: 10.1038/s41598-021-91067-9. PMID: 34075191; PMCID: PMC8169671. 4. Ghosh SP, Kulkarni S, Perkins MW, Hieber K, Pessu RL, Gambles K, Maniar M, Kao TC, Seed TM, Kumar KS. Amelioration of radiation-induced hematopoietic and gastrointestinal damage by Ex-RAD(R) in mice. J Radiat Res. 2012 Jul;53(4):526-36. doi: 10.1093/jrr/rrs001. Epub 2012 Jun 6. PMID: 22843617; PMCID: PMC3393340. |
| In vitro protocol: | 1. Kang AD, Cosenza SC, Bonagura M, Manair M, Reddy MV, Reddy EP. ON01210.Na (Ex-RAD®) mitigates radiation damage through activation of the AKT pathway. PLoS One. 2013;8(3):e58355. doi: 10.1371/journal.pone.0058355. Epub 2013 Mar 7. PMID: 23505494; PMCID: PMC3591351. |
| In vivo protocol: | 1. Li Y, Girgis M, Wise SY, Fatanmi OO, Seed TM, Maniar M, Cheema AK, Singh VK. Analysis of the metabolomic profile in serum of irradiated nonhuman primates treated with Ex-Rad, a radiation countermeasure. Sci Rep. 2021 Jun 1;11(1):11449. doi: 10.1038/s41598-021-91067-9. PMID: 34075191; PMCID: PMC8169671. 2. Ghosh SP, Kulkarni S, Perkins MW, Hieber K, Pessu RL, Gambles K, Maniar M, Kao TC, Seed TM, Kumar KS. Amelioration of radiation-induced hematopoietic and gastrointestinal damage by Ex-RAD(R) in mice. J Radiat Res. 2012 Jul;53(4):526-36. doi: 10.1093/jrr/rrs001. Epub 2012 Jun 6. PMID: 22843617; PMCID: PMC3393340. |
1: Kang AD, Cosenza SC, Bonagura M, Manair M, Reddy MV, Reddy EP. ON01210.Na (Ex-RAD®) mitigates radiation damage through activation of the AKT pathway. PLoS One. 2013;8(3):e58355. doi: 10.1371/journal.pone.0058355. Epub 2013 Mar 7. PubMed PMID: 23505494; PubMed Central PMCID: PMC3591351.
2: Tamhane M, Maniar M, Ren C, Benzeroual KE, Taft DR. Disposition of ON 01210.Na (Ex-RAD(R)), a novel radioprotectant, in the isolated perfused rat liver: probing metabolic inhibition to increase systemic exposure. J Pharm Sci. 2013 Feb;102(2):732-40. doi: 10.1002/jps.23391. Epub 2012 Dec 4. PubMed PMID: 23212688.
3: Ghosh SP, Kulkarni S, Perkins MW, Hieber K, Pessu RL, Gambles K, Maniar M, Kao TC, Seed TM, Kumar KS. Amelioration of radiation-induced hematopoietic and gastrointestinal damage by Ex-RAD(R) in mice. J Radiat Res. 2012 Jul;53(4):526-36. doi: 10.1093/jrr/rrs001. Epub 2012 Jun 6. PubMed PMID: 22843617; PubMed Central PMCID: PMC3393340.
4: Suman S, Datta K, Doiron K, Ren C, Kumar R, Taft DR, Fornace AJ Jr, Maniar M. Radioprotective effects of ON 01210.Na upon oral administration. J Radiat Res. 2012;53(3):368-76. Epub 2012 May 11. PubMed PMID: 22739006.
5: Suman S, Maniar M, Fornace AJ Jr, Datta K. Administration of ON 01210.Na after exposure to ionizing radiation protects bone marrow cells by attenuating DNA damage response. Radiat Oncol. 2012 Jan 20;7:6. doi: 10.1186/1748-717X-7-6. PubMed PMID: 22264334; PubMed Central PMCID: PMC3275448.
6: Bhattacharjee Y. Devastation in Japan. Candidate radiation drugs inch forward. Science. 2011 Mar 25;331(6024):1505. doi: 10.1126/science.331.6024.1505. PubMed PMID: 21436412.
7: Chun AW, Freshwater RE, Taft DR, Gillum AM, Maniar M. Effects of formulation and route of administration on the systemic availability of Ex-RAD®, a new radioprotectant, in preclinical species. Biopharm Drug Dispos. 2011 Mar;32(2):99-111. doi: 10.1002/bdd.741. Epub 2011 Jan 14. PubMed PMID: 21341279.
8: Ghosh SP, Perkins MW, Hieber K, Kulkarni S, Kao TC, Reddy EP, Reddy MV, Maniar M, Seed T, Kumar KS. Radiation protection by a new chemical entity, Ex-Rad: efficacy and mechanisms. Radiat Res. 2009 Feb;171(2):173-9. doi: 10.1667/RR1367.1. PubMed PMID: 19267542.
9: Fernandes PP, Maniar M, Dash AK. Development and validation of a sensitive liquid chromatographic method for the analysis of a novel radioprotectant: ON 01210.Na. J Pharm Biomed Anal. 2007 Apr 11;43(5):1796-803. Epub 2006 Dec 20. PubMed PMID: 17184951.
