RO5045337
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MedKoo CAT#: 202421

CAS#: 939981-39-2

Description: RO5045337, also known as RG7112, is a MDM2 antagonist with potential antineoplastic activity. RO5045337 binds to MDM2, thereby preventing the binding of the MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this MDM2-p53 interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited and the transcriptional activity of p53 is restored, which may result in the restoration of p53 signaling and thus the p53-mediated induction of tumor cell apoptosis. MDM2, a zinc finger protein, is a negative regulator of the p53 pathway; often overexpressed in cancer cells, it has been implicated in cancer cell proliferation and survival.


Price and Availability

Size
Price

10mg
USD 250
100mg
USD 950
1g
USD 3450
Size
Price

25mg
USD 450
200mg
USD 1650
2g
USD 4650
Size
Price

50mg
USD 650
500mg
USD 2150
5g
Ask price

RO5045337, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 202421
Name: RO5045337
CAS#: 939981-39-2
Chemical Formula: C38H48Cl2N4O4S
Exact Mass: 726.27733
Molecular Weight: 727.78
Elemental Analysis: C, 62.71; H, 6.65; Cl, 9.74; N, 7.70; O, 8.79; S, 4.41


Synonym: R7112 RG7112 RG 7112; RG7112; RO5045337; RO 5045337; RO5045337

IUPAC/Chemical Name: ((4S,5R)-2-(4-(tert-butyl)-2-ethoxyphenyl)-4,5-bis(4-chlorophenyl)-4,5-dimethyl-4,5-dihydro-1H-imidazol-1-yl)(4-(3-(methylsulfonyl)propyl)piperazin-1-yl)methanone

InChi Key: QBGKPEROWUKSBK-QPPIDDCLSA-N

InChi Code: InChI=1S/C38H48Cl2N4O4S/c1-8-48-33-26-29(36(2,3)4)14-19-32(33)34-41-37(5,27-10-15-30(39)16-11-27)38(6,28-12-17-31(40)18-13-28)44(34)35(45)43-23-21-42(22-24-43)20-9-25-49(7,46)47/h10-19,26H,8-9,20-25H2,1-7H3/t37-,38+/m0/s1

SMILES Code: O=C(N1[C@](C)(C2=CC=C(Cl)C=C2)[C@](C)(C3=CC=C(Cl)C=C3)N=C1C4=CC=C(C(C)(C)C)C=C4OCC)N5CCN(CCCS(=O)(C)=O)CC5


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

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).

Harmonized System Code:
293490


Additional Information

  
   
 
 


References

1: Ding Q, Zhang Z, Liu JJ, Jiang N, Zhang J, Ross TM, Chu XJ, Bartkovitz D, Podlaski F, Janson C, Tovar C, Filipovic ZM, Higgins B, Glenn K, Packman K, Vassilev LT, Graves B. Discovery of RG7388, a Potent and Selective p53-MDM2 Inhibitor in Clinical Development. J Med Chem. 2013 Jul 16. [Epub ahead of print] PubMed PMID: 23808545.

2: Tovar C, Graves B, Packman K, Filipovic Z, Higgins B, Xia M, Tardell C, Garrido R, Lee E, Kolinsky K, To KH, Linn M, Podlaski F, Wovkulich P, Vu B, Vassilev LT. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res. 2013 Apr 15;73(8):2587-97. doi: 10.1158/0008-5472.CAN-12-2807. Epub 2013 Feb 11. PubMed PMID: 23400593.

3: Ray-Coquard I, Blay JY, Italiano A, Le Cesne A, Penel N, Zhi J, Heil F, Rueger R, Graves B, Ding M, Geho D, Middleton SA, Vassilev LT, Nichols GL, Bui BN. Effect of the MDM2 antagonist RG7112 on the P53 pathway in patients with MDM2-amplified, well-differentiated or dedifferentiated liposarcoma: an exploratory proof-of-mechanism study. Lancet Oncol. 2012 Nov;13(11):1133-40. doi: 10.1016/S1470-2045(12)70474-6. Epub 2012 Oct 17. PubMed PMID: 23084521.

4: Carol H, Reynolds CP, Kang MH, Keir ST, Maris JM, Gorlick R, Kolb EA, Billups CA, Geier B, Kurmasheva RT, Houghton PJ, Smith MA, Lock RB. Initial testing of the MDM2 inhibitor RG7112 by the Pediatric Preclinical Testing Program. Pediatr Blood Cancer. 2013 Apr;60(4):633-41. doi: 10.1002/pbc.24235. Epub 2012 Jul 2. PubMed PMID: 22753001; PubMed Central PMCID: PMC3495996.

5: Millard M, Pathania D, Grande F, Xu S, Neamati N. Small-molecule inhibitors of p53-MDM2 interaction: the 2006-2010 update. Curr Pharm Des. 2011;17(6):536-59. Review. PubMed PMID: 21391905.