NVP-CGM097 free base | CAS#1313363-54-0 | MDM2 inhibitor

MedKoo Cat#: 207222 | Name: NVP-CGM097 free base

Description:

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

NVP-CGM097 is a potent and selective MDM2 inhibitor. P53 wild type GOT1 cells were sensitive to NVP-CGM097, p53mutated BON1 and p53mutated NCI-H727 cells were resistant to NVP-CGM097. Incubation of GOT1 cells with NVP-CGM097 at 100, 500, and 2,500 nM for 96 h caused a significant decline in cell viability to 84.9 ± 9.2% (p < 0.05), 77.4 ± 6.6% (p < 0.01), and 47.7 ± 9.2% (p < 0.01). NVP-CGM097 can inhibit the proliferation of tumor cells. NVP-CGM097 could reverse ABCB1-mediated MDR by directly blocking the ABCB1-mediated drug efflux and raising the accumulation of chemotherapeutic drugs in cancer cells. NVP-CGM097 tended to bind to the inhibitory site, which led to slight but critical conformational changes in the transporter and reduced the ATPase activity.

Chemical Structure

NVP-CGM097 free base

CAS#1313363-54-0 (free base)

Theoretical Analysis

MedKoo Cat#: 207222

Name: NVP-CGM097 free base

CAS#: 1313363-54-0 (free base)

Chemical Formula: C38H47ClN4O4

Exact Mass: 658.3286

Molecular Weight: 659.27

Elemental Analysis: C, 69.23; H, 7.19; Cl, 5.38; N, 8.50; O, 9.71

Price and Availability

Size	Price	Availability
10mg	USD 450.00	2 Weeks
25mg	USD 850.00	2 Weeks
50mg	USD 1,250.00	2 Weeks
100mg	USD 2,050.00	2 Weeks

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Related CAS #

1313363-54-0 (free base) 1313367-56-4 (sulfate)

Synonym

NVP-CGM097 free base; NVP CGM097; NVP-CGM 097; NVP-CGM-097; NVPCGM097; NVPCGM 097; NVPCGM-097; CGM 097; CGM-097; CGM097;

IUPAC/Chemical Name

(S)-1-(4-chlorophenyl)-7-isopropoxy-6-methoxy-2-(4-(methyl(((1r,4S)-4-(4-methyl-3-oxopiperazin-1-yl)cyclohexyl)methyl)amino)phenyl)-1,4-dihydroisoquinolin-3(2H)-one

InChi Key

CLRSLRWKONPSRQ-IIPSPAQQSA-N

InChi Code

InChI=1S/C38H47ClN4O4/c1-25(2)47-35-22-33-28(20-34(35)46-5)21-36(44)43(38(33)27-8-10-29(39)11-9-27)32-16-14-30(15-17-32)41(4)23-26-6-12-31(13-7-26)42-19-18-40(3)37(45)24-42/h8-11,14-17,20,22,25-26,31,38H,6-7,12-13,18-19,21,23-24H2,1-5H3/t26-,31-,38-/m0/s1

SMILES Code

O=C1N(C2=CC=C(N(C)C[C@H]3CC[C@H](N4CC(N(C)CC4)=O)CC3)C=C2)[C@@H](C5=CC=C(Cl)C=C5)C6=C(C=C(OC)C(OC(C)C)=C6)C1

Appearance

To be determined

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 659.27 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

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The MDM2 inhibitor CGM097 combined with the BET inhibitor OTX015 induces cell death and inhibits tumor growth in models of neuroblastoma. Cancer Med. 2020 Nov;9(21):8144-8158. doi: 10.1002/cam4.3407. Epub 2020 Oct 9. PMID: 33034426; PMCID: PMC7643634. 7: Fang Y, Liao G, Yu B. Small-molecule MDM2/X inhibitors and PROTAC degraders for cancer therapy: advances and perspectives. Acta Pharm Sin B. 2020 Jul;10(7):1253-1278. doi: 10.1016/j.apsb.2020.01.003. Epub 2020 Jan 14. PMID: 32874827; PMCID: PMC7452049. 8: Zhang M, Chen XY, Dong XD, Wang JQ, Feng W, Teng QX, Cui Q, Li J, Li XQ, Chen ZS. NVP-CGM097, an HDM2 Inhibitor, Antagonizes ATP-Binding Cassette Subfamily B Member 1-Mediated Drug Resistance. Front Oncol. 2020 Jul 23;10:1219. doi: 10.3389/fonc.2020.01219. PMID: 32793491; PMCID: PMC7390918. 9: Portman N, Milioli HH, Alexandrou S, Coulson R, Yong A, Fernandez KJ, Chia KM, Halilovic E, Segara D, Parker A, Haupt S, Haupt Y, Tilley WD, Swarbrick A, Caldon CE, Lim E. MDM2 inhibition in combination with endocrine therapy and CDK4/6 inhibition for the treatment of ER-positive breast cancer. Breast Cancer Res. 2020 Aug 12;22(1):87. doi: 10.1186/s13058-020-01318-2. PMID: 32787886; PMCID: PMC7425060. 10: Konopleva M, Martinelli G, Daver N, Papayannidis C, Wei A, Higgins B, Ott M, Mascarenhas J, Andreeff M. MDM2 inhibition: an important step forward in cancer therapy. Leukemia. 2020 Nov;34(11):2858-2874. doi: 10.1038/s41375-020-0949-z. Epub 2020 Jul 10. PMID: 32651541. 11: de Koning L, Decaudin D, El Botty R, Nicolas A, Carita G, Schuller M, Ouine B, Cartier A, Naguez A, Fleury J, Cooke V, Wylie A, Smith P, Marangoni E, Gentien D, Meseure D, Mariani P, Cassoux N, Piperno-Neumann S, Roman-Roman S, Némati F. PARP Inhibition Increases the Response to Chemotherapy in Uveal Melanoma. Cancers (Basel). 2019 May 29;11(6):751. doi: 10.3390/cancers11060751. PMID: 31146482; PMCID: PMC6628115. 12: Kallen J, Izaac A, Chau S, Wirth E, Schoepfer J, Mah R, Schlapbach A, Stutz S, Vaupel A, Guagnano V, Masuya K, Stachyra TM, Salem B, Chene P, Gessier F, Holzer P, Furet P. Structural States of Hdm2 and HdmX: X-ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes. ChemMedChem. 2019 Jul 17;14(14):1305-1314. doi: 10.1002/cmdc.201900201. Epub 2019 May 27. PMID: 31066983. 13: Tan B, Tong C, Yuan Y, Xu P, Wen L, Zhang C, Zheng Y, Lin L, Zhu F, Gui S, Wang L, Gao R, Li J, Qi H, Baker PN. The Regulation of Trophoblastic p53 Homeostasis by the p38-Wip1 Feedback Loop is Disturbed in Placentas from Pregnancies Complicated by Preeclampsia. Cell Physiol Biochem. 2019;52(2):315-335. doi: 10.33594/000000023. Epub 2019 Feb 28. PMID: 30816677. 14: Liao G, Yang D, Ma L, Li W, Hu L, Zeng L, Wu P, Duan L, Liu Z. The development of piperidinones as potent MDM2-P53 protein-protein interaction inhibitors for cancer therapy. 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The HDM2 (MDM2) Inhibitor NVP-CGM097 Inhibits Tumor Cell Proliferation and Shows Additive Effects with 5-Fluorouracil on the p53-p21-Rb-E2F1 Cascade in the p53wild type Neuroendocrine Tumor Cell Line GOT1. Neuroendocrinology. 2018;106(1):1-19. doi: 10.1159/000453369. Epub 2016 Nov 21. PMID: 27871087. 18: Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D. Correction: A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097. Elife. 2016 Nov 17;5:e19317. doi: 10.7554/eLife.19317. Erratum for: Elife. 2015 May 12;4:e06498. doi: 10.7554/eLife.06498. PMID: 27852439; PMCID: PMC5114012. 19: Furet P, Masuya K, Kallen J, Stachyra-Valat T, Ruetz S, Guagnano V, Holzer P, Mah R, Stutz S, Vaupel A, Chène P, Jeay S, Schlapbach A. 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