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939981-39-2 (RG7112)

1

Identification

RG7112 RG7112
Name RG7112
Formula C38H48Cl2N4O4S
MW 727.78
CAS No. 939981-39-2
EINECS
Smiles C[[email protected]@]1([[email protected]](C)(N(C(C2=CC=C(C=C2OCC)C(C)(C)C)=N1)C(N3CCN(CC3)CCCS(=O)(C)=O)=O)C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
Synonyms RG-7112;RG 7112; ((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 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
2

Introduction

RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. IC50 Value: Target: MDM2/p53 Restoration of p53 activity by inhibiting the p53-MDM2 interaction may represent a novel approach to cancer treatment.

Background Information

The first small-molecule for MDM2 inhibitor designed to occupy the p53-binding pocket. ......by AOBIOUS INC
RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. In cancer cells expressing wild-type p53, RG7112 stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts. ......by AbMole BioScience
RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2. ......by AdooQ BioScience, LLC
Description ......by Apexbio Technology LLC
RO5045337, also known as R7112, 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 BOC Sciences
RG-7112 is a Nutlin imidazoline compound that acts as a potent MDM2 inhibitor as well as displays antineoplastic activity. RG-7112 binds to MDM2, thereby preventing the binding of the MDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. ......by BioVision, Inc.,
RG7112 is the first clinical and orally available MDM-2/p53 inhibitor designed to occupy the p53-binding pocket of MDM2, with the Kd value of 11 nM. ......by MedChemexpress Co., Ltd.
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. ......by MedKoo Biosciences, Inc.
A potent and selective inhibitor of p53-MDM2 interaction; binds MDM2 with high affinity (Kd=11 nM); stabilizes p53 and activates the p53 pathway, leading to cell cycle arrest, apoptosis, and inhibition or regression of human tumor xenografts. orally bioactive. ......by ProbeChem
RG7112 (RO5045337) is an orally bioavailable and selective p53-MDM2 inhibitor with HTRF IC50 of 18 nM. ......by Selleck Chemicals LLC
3

Protocol(Only for Reference)

Cell Experiment

Cell lines SJSA1 osteosarcoma cells
Conditions 24 h; 10 μM
Method Treatment of cultured cancer cells with RG7112 led to concentration-dependent accumulation of p53 protein and its transcriptional targets, p21 and MDM2. RG7112 dose dependently inhibited the growth and killed SJSA1 osteosarcoma cells expressing high-levels of MDM2 protein due to MDM2 gene ampli fication
Source Apexbio Technology LLC

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000028836

Storage condition

Store at -20°C by Apexbio Technology LLC

Solubility

Soluble in DMSO by Apexbio Technology LLC
DMSO by MedChemexpress Co., Ltd.
5

Mechanism and Indication

6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
RG7112 Roche Holding AG Acute myelogenous leukemia 2012/7/31 2013/9/30 Phase 1 Clinical
RG7112 Roche Holding AG Soft tissue sarcoma 2012/5/31 2013/8/31 Phase 1 Clinical
RG7112 Roche Holding AG Cancer 2012/11/30 2014/8/31 Phase 1 Clinical
RG7112 Roche Holding AG Solid tumor 2010/8/31 2013/5/1 Phase 1 Clinical
RG7112 Roche Holding AG Liposarcoma 2010/6/30 2011/3/1 Phase 1 Clinical
RG7112 - No Development Reported
7

Safety Data of RG7112

8

Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AOBIOUS INC USA
AbMole BioScience USA
AdooQ BioScience, LLC USA
Apexbio Technology LLC USA
Ark Pharm, Inc. USA
BOC Sciences
BioVision, Inc., USA
Biochempartner Co., Ltd China
CHEMSCENE, LLC 5mg/USD144();10mg/USD252() USA
MedChemexpress Co., Ltd. 5mg/USD144();10mg/USD252() USA
MedKoo Biosciences, Inc. USA
ProbeChem
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD144();10mg/USD252() China
10

Related Products

Other Forms of 939981-39-2

Name CAS No Formula MW
RG7112 Racemate 1313611-29-8 C38H48Cl2N4O4S 727.7831

Recommended Compounds in MDM-2/p53

Name CAS No Formula MW
YH239-EE 1364488-67-4 C25H27Cl2N3O4 504.41
SJ-172550 431979-47-4 C22H21ClN2O5 428.87
NVP-CGM097 1313363-54-0 C38H47ClN4O4 659.26
Tenovin 6 (Hydrochloride) 1011301-29-3 C25H35ClN4O2S 491.09
MI-773 1303607-07-9 C29H34Cl2FN3O3 562.5
Puromycin aminonucleoside 58-60-6 C12H18N6O3 294.31
RG7388 1229705-06-9 C31H29Cl2F2N3O4 616.48
Solasodine 126-17-0 C27H43NO2 413.64
RITA 213261-59-7 C14H12O3S2 292.37
Tenovin-6 1011557-82-6 C25H34N4O2S 454.63
Pifithrin-α (hydrobromide) 63208-82-2 C16H19BrN2OS 367.3
Kevetrin (hydrochloride) 66592-89-0 C5H10ClN3S 179.671
Nutlin (3b) 675576-97-3 C30H30Cl2N4O4 581.4896
p53 and MDM2 proteins-interaction-inhibitor (chiral) 939981-37-0 C40H49Cl2N5O4 734.75
p53 and MDM2 proteins-interaction-inhibitor (chiral) 939981-37-0 C40H49Cl2N5O4 734.7542
Nutlin (3a) 675576-98-4 C30H30Cl2N4O4 581.4896
Nutlin (3b) 675576-97-3 C30H30Cl2N4O4 581.4896
Triptolide 38748-32-2 C20H24O6 360.4
Serdemetan 881202-45-5 C21H20N4 328.41
PRIMA-1Met 5291-32-7 C10H17NO3 199.2469

Recommended Compounds in Same Indication

Name CAS No Formula MW
AZD1152 722543-31-9 C26H31FN7O6P 587.54
AZD1152-HQPA 722544-51-6 C26H30FN7O3 507.56
Mocetinostat 726169-73-9 C23H20N6O 396.44
Volasertib 755038-65-4 C34H50N8O3 618.81
PU-H71 873436-91-0 C18H21IN6O2S 512.37
BMS-599626 (Hydrochloride) 873837-23-1 C27H28ClFN8O3 567.01
AT9283 896466-04-9 C19H23N7O2 381.43
KX2-391 897016-82-9 C26H29N3O3 431.53
MLN4924 905579-51-3 C21H25N5O4S 443.52
SNX-2112 908112-43-6 C23H27F3N4O3 464.48
Nordihydroguaiaretic acid 500-38-9 C18H22O4 302.36
Pazopanib (Hydrochloride) 635702-64-6 C21H24ClN7O2S 473.98
RX-3117 865838-26-2 C10H12FN3O4 257.22
Crenolanib 670220-88-9 C26H29N5O2 443.54
OSU-03012 742112-33-0 C26H19F3N4O 460.45
Retaspimycin 857402-23-4 C31H45N3O8 587.7
Retaspimycin (Hydrochloride) 857402-63-2 C31H46ClN3O8 624.17
Motesanib (Diphosphate) 857876-30-3 C22H29N5O9P2 569.44
Octreotide (acetate) 79517-01-4 C51H70N10O12S2 1079.29
LY2603618 911222-45-2 C18H22BrN5O3 436.3
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Route of Synthesis

12

References

[1]. Vu, Binh; Wovkulich, Peter; Pizzolato, Giacomo et al. Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. ACS Medicinal Chemistry Letters (2013), 4(5), 466-469.

Protocol Reference

[1] Tovar C, Graves B, Packman K, et al. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models[J]. Cancer research, 2013, 73(8): 2587-2597.

......by Apexbio Technology LLC
13

More Information

RG7112

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