Roslin 2 | CAS#29574-21-8 | p53 reactivator

MedKoo Cat#: 341200 | Name: Roslin 2 Bromide

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Description:

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

Roslin 2 is a p53 reactivator that disrupts the FAK and p53 interaction, and reactivates transcriptional activity of p53 with p21, Mdm-2 and Bax transcriptional targets. Roslin 2 decreases viability and clonogenicity of cancer cells, and inhibits tumor growth.

Chemical Structure

Roslin 2 Bromide

CAS#29574-21-8

Theoretical Analysis

MedKoo Cat#: 341200

Name: Roslin 2 Bromide

CAS#: 29574-21-8

Chemical Formula: C13H19BrN4

Exact Mass: 310.0793

Molecular Weight: 311.23

Elemental Analysis: C, 50.17; H, 6.15; Br, 25.67; N, 18.00

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 225.00
25mg	USD 550.00

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Synonym

Roslin 2; Roslin-2; Roslin2.

IUPAC/Chemical Name

1-(Phenylmethyl)-3,5,7-triaza-1-azoniatricyclo[3.3.1.1~3,7~]decane bromide, 1-Benzyl-1,3,5,7-tetraazatricyclo[3.3.1.1~3,7~] decane bromide, 1-Benzyl-3,5,7-triaza-1-azoniaadamantane bromide

InChi Key

YJMKPGPWDHCYCD-UHFFFAOYSA-M

InChi Code

InChI=1S/C13H19N4.BrH/c1-2-4-13(5-3-1)6-17-10-14-7-15(11-17)9-16(8-14)12-17;/h1-5H,6-12H2;1H/q+1;/p-1

SMILES Code

N12C[N+](C3)(CC4=CC=CC=C4)CN(C2)CN3C1.[Br-]

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

To be determined

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

Instruction

View handling instruction

Biological target:

Roslin-2 impairs the interaction between focal adhesion kinase (FAK) and p53 and restores p53 transcriptional activity. It reverses FAK-mediated suppression of the expression of p53-dependent p21, MDM2, and Bax in wild-type p53 HCT116 colon and MCF-7 breast cancer cells. Roslin-2 reduces tumor growth and activates p21 in p53+/+, in HCT116 mouse xenograft models.

In vitro activity:

Roslin-2 increased p53 transcriptional activity that was inhibited by FAK using p21, Mdm-2, and Bax-promoter targets. Roslin-2 also caused increased expression of p53 targets: p21, Mdm-2 and Bax proteins. Reference: BMC Cancer. 2013 Jul 11;13:342. https://pubmed.ncbi.nlm.nih.gov/23841915/

In vivo activity:

Roslin-2 significantly decreased tumor growth, disrupted the complex of FAK and p53, and up-regulated p21 in HCT116 p53+/+ but not in HCT116 p53-/- xenografts in vivo. Roslin-2 also sensitized HCT116p53+/+ cells to doxorubicin and 5-fluorouracil. Reference: BMC Cancer. 2013 Jul 11;13:342. https://pubmed.ncbi.nlm.nih.gov/23841915/

Preparing Stock Solutions

The following data is based on the product molecular weight 311.23 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. Golubovskaya VM, Ho B, Zheng M, Magis A, Ostrov D, Morrison C, Cance WG. Disruption of focal adhesion kinase and p53 interaction with small molecule compound R2 reactivated p53 and blocked tumor growth. BMC Cancer. 2013 Jul 11;13:342. doi: 10.1186/1471-2407-13-342. PMID: 23841915; PMCID: PMC3712010.

In vitro protocol:

In vivo protocol:

1: Learmount J, Callaby R, Taylor M. An observational study of ewe treatments at lambing on early infection in lambs on UK sheep farms. Vet Parasitol. 2018 Apr 15;253:55-59. doi: 10.1016/j.vetpar.2018.02.026. Epub 2018 Feb 12. PubMed PMID: 29605004. 2: Takahashi M, McCartney E, Knox A, Francesch M, Oka K, Wada K, Ideno M, Uno K, Kozłowski K, Jankowski J, Gracia MI, Morales J, Kritas SK, Esteve-Garcia E, Kamiya S. Effects of the butyric acid-producing strain Clostridium butyricum MIYAIRI 588 on broiler and piglet zootechnical performance and prevention of necrotic enteritis. Anim Sci J. 2018 Mar 30. doi: 10.1111/asj.13006. [Epub ahead of print] PubMed PMID: 29603498. 3: Amengual Batle P, Rusbridge C, Nuttall T, Heath S, Marioni-Henry K. Feline hyperaesthesia syndrome with self-trauma to the tail: retrospective study of seven cases and proposal for integrated multidisciplinary diagnostic approach. J Feline Med Surg. 2018 Mar 1:1098612X18764246. doi: 10.1177/1098612X18764246. [Epub ahead of print] PubMed PMID: 29595359. 4: Porphyre T, Rich KM, Auty HK. Assessing the Economic Impact of Vaccine Availability When Controlling Foot and Mouth Disease Outbreaks. Front Vet Sci. 2018 Mar 13;5:47. doi: 10.3389/fvets.2018.00047. eCollection 2018. PubMed PMID: 29594161; PubMed Central PMCID: PMC5859371. 5: Palaiokostas C, Kocour M, Prchal M, Houston RD. Accuracy of Genomic Evaluations of Juvenile Growth Rate in Common Carp (Cyprinus carpio) Using Genotyping by Sequencing. Front Genet. 2018 Mar 13;9:82. doi: 10.3389/fgene.2018.00082. eCollection 2018. PubMed PMID: 29593780; PubMed Central PMCID: PMC5859378. 6: Lam WL, Oh JDH, Johnson EJ, Pertinez SP, Stephens C, Davey MG. Experimental evidence that preaxial polydactyly and forearm radial deficiencies may share a common developmental origin. J Hand Surg Eur Vol. 2018 Jan 1:1753193418762959. doi: 10.1177/1753193418762959. [Epub ahead of print] PubMed PMID: 29587601. 7: Roach RC, Hackett PH, Oelz O, Bärtsch P, Luks AM, MacInnis MJ, Baillie JK; Lake Louise AMS Score Consensus Committee. The 2018 Lake Louise Acute Mountain Sickness Score. High Alt Med Biol. 2018 Mar;19(1):4-6. doi: 10.1089/ham.2017.0164. Epub 2018 Mar 13. PubMed PMID: 29583031. 8: Martin JE, Sandercock DA, Sandilands V, Sparrey J, Baker L, Sparks NHC, McKeegan DEF. Welfare Risks of Repeated Application of On-Farm Killing Methods for Poultry. Animals (Basel). 2018 Mar 15;8(3). pii: E39. doi: 10.3390/ani8030039. PubMed PMID: 29543779; PubMed Central PMCID: PMC5867527. 9: Surve A, Cottam D, Sanchez-Pernaute A, Torres A, Roller J, Kwon Y, Mourot J, Schniederjan B, Neichoy B, Enochs P, Tyner M, Bruce J, Bovard S, Roslin M, Jawad M, Teixeira A, Srikanth M, Free J, Zaveri H, Pilati D, Bull J, Belnap L, Richards C, Medlin W, Moon R, Cottam A, Sabrudin S, Cottam S, Dhorepatil A. The incidence of complications associated with loop duodeno-ileostomy after single-anastomosis duodenal switch procedures among 1328 patients: a multicenter experience. Surg Obes Relat Dis. 2018 Feb 2. pii: S1550-7289(18)30035-2. doi: 10.1016/j.soard.2018.01.020. [Epub ahead of print] PubMed PMID: 29530597. 10: Maroso F, Hillen JEJ, Pardo BG, Gkagkavouzis K, Coscia I, Hermida M, Franch R, Hellemans B, Van Houdt J, Simionati B, Taggart JB, Nielsen EE, Maes G, Ciavaglia SA, Webster LMI, Volckaert FAM, Martinez P, Bargelloni L, Ogden R; AquaTrace Consortium. Performance and precision of double digestion RAD (ddRAD) genotyping in large multiplexed datasets of marine fish species. Mar Genomics. 2018 Feb 27. pii: S1874-7787(17)30141-1. doi: 10.1016/j.margen.2018.02.002. [Epub ahead of print] PubMed PMID: 29496460. 11: Airikkala-Otter I, Gamble L, Mazeri S, Handel IG, Bronsvoort BMC, Mellanby RJ, Meunier NV. Investigation of short-term surgical complications in a low-resource, high-volume dog sterilisation clinic in India. BMC Vet Res. 2018 Feb 27;14(1):56. doi: 10.1186/s12917-018-1378-3. PubMed PMID: 29482640; PubMed Central PMCID: PMC5828070. 12: Cartwright JA, Gow AG, Milne E, Drummond D, Smith S, Handel I, Mellanby RJ. Vitamin D Receptor Expression in Dogs. J Vet Intern Med. 2018 Mar;32(2):764-774. doi: 10.1111/jvim.15052. Epub 2018 Feb 22. PubMed PMID: 29469965; PubMed Central PMCID: PMC5866978. 13: Farnworth MJ, Packer RMA, Sordo L, Chen R, Caney SMA, Gunn-Moore DA. In the Eye of the Beholder: Owner Preferences for Variations in Cats' Appearances with Specific Focus on Skull Morphology. Animals (Basel). 2018 Feb 20;8(2). pii: E30. doi: 10.3390/ani8020030. PubMed PMID: 29461472; PubMed Central PMCID: PMC5836038. 14: Mantsoki A, Devailly G, Joshi A. Dynamics of promoter bivalency and RNAP II pausing in mouse stem and differentiated cells. BMC Dev Biol. 2018 Feb 20;18(1):2. doi: 10.1186/s12861-018-0163-7. PubMed PMID: 29458328; PubMed Central PMCID: PMC5819258. 15: Robinson LM, Coleman K, Capitanio JP, Gottlieb DH, Handel IG, Adams MJ, Leach MC, Waran NK, Weiss A. Rhesus macaque personality, dominance, behavior, and health. Am J Primatol. 2018 Feb;80(2). doi: 10.1002/ajp.22739. Epub 2018 Feb 19. PubMed PMID: 29457637. 16: Seeker LA, Ilska JJ, Psifidi A, Wilbourn RV, Underwood SL, Fairlie J, Holland R, Froy H, Bagnall A, Whitelaw B, Coffey M, Nussey DH, Banos G. Longitudinal changes in telomere length and associated genetic parameters in dairy cattle analysed using random regression models. PLoS One. 2018 Feb 13;13(2):e0192864. doi: 10.1371/journal.pone.0192864. eCollection 2018. PubMed PMID: 29438415; PubMed Central PMCID: PMC5811042. 17: Alderton S, Macleod ET, Anderson NE, Palmer G, Machila N, Simuunza M, Welburn SC, Atkinson PM. An agent-based model of tsetse fly response to seasonal climatic drivers: Assessing the impact on sleeping sickness transmission rates. PLoS Negl Trop Dis. 2018 Feb 9;12(2):e0006188. doi: 10.1371/journal.pntd.0006188. eCollection 2018 Feb. PubMed PMID: 29425200; PubMed Central PMCID: PMC5806852. 18: Robledo D, Matika O, Hamilton A, Houston RD. Genome-Wide Association and Genomic Selection for Resistance to Amoebic Gill Disease in Atlantic Salmon. G3 (Bethesda). 2018 Mar 28;8(4):1195-1203. doi: 10.1534/g3.118.200075. PubMed PMID: 29420190; PubMed Central PMCID: PMC5873910. 19: McGorum BC, Pirie RS. Equine Dysautonomia. Vet Clin North Am Equine Pract. 2018 Apr;34(1):113-125. doi: 10.1016/j.cveq.2017.11.010. Epub 2018 Feb 3. Review. PubMed PMID: 29398183. 20: Downs SH, Parry JE, Upton PA, Broughan JM, Goodchild AV, Nuñez-Garcia J, Greiner M, Abernethy DA, Cameron AR, Cook AJ, de la Rua-Domenech R, Gunn J, Pritchard E, Rhodes S, Rolfe S, Sharp M, Vordermeier HM, Watson E, Welsh M, Whelan AO, Woolliams JA, More SJ, Clifton-Hadley RS. Methodology and preliminary results of a systematic literature review of ante-mortem and post-mortem diagnostic tests for bovine tuberculosis. Prev Vet Med. 2017 Nov 9. pii: S0167-5877(17)30023-5. doi: 10.1016/j.prevetmed.2017.11.004. [Epub ahead of print] PubMed PMID: 29395122.