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NVP-CGM097

NVP-CGM097

Catalog No.

B4677

potent and selective MDM2 inhibitor

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Grouped product items
Size	Price	Stock	Qty
2mg	$198.00	Ship with 10-15 days
5mg	$348.00	Ship with 10-15 days
10mg	$595.00	Ship with 10-15 days
50mg	$2,315.00	Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

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Chemical Properties
Protocol
Quality Control

Chemical Properties

Storage	Store at -20°C
M.Wt	659.26
Cas No.	1313363-54-0
Formula	C₃₈H₄₇ClN₄O₄
Solubility	Soluble in DMSO
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)-1,2-dihydroisoquinolin-3(4H)-one
SDF	Download SDF
Canonical SMILES	CC(OC(C=C1[C@]2([H])C3=CC=C(Cl)C=C3)=C(OC)C=C1CC(N2C4=CC=C(N(C[C@@]5([H])CC[C@@](N(CC6=O)CCN6C)([H])CC5)C)C=C4)=O)C
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment [1,2]:
Cell lines	Neuroblastoma cell lines, HCT116 cells
Preparation method	Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	24 h
Applications	The combination of NVP-CGM097 with NVP-LDK378 promoted apoptosis in ALK mutant and p53 WT neuroblastoma cell lines. NVP-LDK378 inhibited ALK phosphorylation and NVP-CGM097 caused induction of p53 and its downstream target genes in these cell lines. NVP-CGM097 significantly inhibited the proliferation of cells expressing wild-type p53, while sparing the p53 null cells with a 35-58-fold difference. NVP-CGM097 significantly redistributed wild-type p53 into the cell nucleus with an IC50 of 0.224 μM. NVP-CGM097 inhibited HCT116 (p53WT/WT) with IC50 of 454 ± 136 nM.
Animal experiment [1,3]:
Animal models	NOD.SCID.IL2R-/- (NSG) mice engraftmented with hCD45+/hCD19+ cells, ALK mutant neuroblastoma models, MDM2-amplified SJSA-1 human tumor model
Dosage form	Intravenous injection, 30 mg/kg, Daily
Application	In NOD.SCID.IL2R-/- (NSG) mice engraftmented with hCD45+/hCD19+ cells, CGM097 ultimately became moribund from progressive leukemia. CGM097 significantly upregulated the expression of 11 genes at the 26 hour timepoint, including the canonical p53 targets BBC3, CDKN1A and MDM2. CGM097 markedly improved overall survival. NVP-LDK378 and NVP-CGM097 combination resulted in complete tumor regression and markedly prolonged survival in neuroblastoma xenograft models. NVP-CGM097 inhibited the interaction between p53 and MDM2 and reactivated the p53 pathway in a MDM2-amplified SJSA-1 human tumor model. NVP-CGM097 (30 mg/kg) increased p21 mRNA levels in tumor-bearing rats. Daily treatment with NVP-CGM097 dose-dependently inhibited SJSA-1 tumor growth in rats.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References: [1]. Wang H Q, Battalagine L, Liang J, et al. The Mdm2 inhibitor NVP-CGM097 enhances the anti-tumor activity of NVP-LDK378 in ALK mutant neuroblastoma models[J]. 2014. [2]. Holzer P, et al. Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. J Med Chem. 2015 Aug 27;58(16):6348-58. [3]. Townsend E C, DeSouza T, Murakami M A, et al. The MDM2 Inhibitor NVP-CGM097 Is highly active in a randomized preclinical trial of B-cell acute lymphoblastic leukemia patient derived xenografts[J]. 2015.

Quality Control

Quality Control & MSDS

View current batch:

Purity = 98.00%

COA (Certificate Of Analysis)
MSDS (Material Safety Data Sheet)

Chemical structure

NVP-CGM097