NVP-CGM097
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $1340 | Check With Us |
| 500mg | $1950 | Check With Us |
| 1g | $2925 | Check With Us |
: Cat #: V2654 CAS #: 1313363-54-0 Purity ≥ 98%
Description: NVP-CGM097 (also called CGM-097; CGM097; NVP-CGM-097; NVP CGM097) is a novel, highly potent, orally bioavailable and selective MDM2 ( (human homolog of double minute 2) inhibitor with antitumor activity.
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| Molecular Weight (MW) | 659.26 |
|---|---|
| Molecular Formula | C38H47ClN4O4 |
| CAS No. | 1313363-54-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 65 mg/mL (98.6 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 65 mg/mL (98.6 mM) | |
| 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 |
| Synonyms | CGM-097, CGM097, CGM 097, NVP CGM097; CGM097; CGM-097; CGM 097; NVPCGM097; NVPCGM 097; NVPCGM-097; NVP CGM097; NVP CGM 097; NVP CGM-097. |
| Protocol | In Vitro | NVP-CGM097 binds to human MDM2 with an IC50 of 1.7 nM and shows high selectivity over MDM4 (IC50=2000 nM). NVP-CGM097 is about four times more potent than Nutlin-3a (IC50=8 nM). In addition, NVP-CGM097 shows no significant activity against Bcl-2:Bak, Bcl-2:Bad, Mcl-1:Bak, Mcl-1:NOXA, XIAP:BIR3, and c-IAP:BIR3 protein-protein interactions. NVP-CGM097 significantly inhibits the proliferation of cells expressing wild-type p53, while sparing the p53 null cells with a 35-58-fold difference. NVP-CGM097 is able to significantly redistribute wild-type p53 into the cell nucleus with an IC50 of 0.224 μM, demonstrating its ability to inhibit the p53:MDM2 interaction in living cells. In addition, NVP-CGM097 activity against the p53:MDM2 interaction is assessed in proliferation assays using either wild-type p53 or p53 null cells. NVP-CGM097 significantly inhibits the proliferation of cells expressing wild-type p53, while sparing the p53 null cells with a 35-58-fold difference. NVP-CGM097 inhibtis HCT116 (p53WT/WT) with IC50 of 454±136 nM. |
|---|---|---|
| In Vivo | NVP-CGM097 is able to inhibit the interaction between p53 and MDM2 and reactivate the p53 pathway in vivo in a MDM2-amplified SJSA-1 human tumor model, as judged by elevation of p21 mRNA levels, a pharmacodynamic (PD) indicator for p53 activity. p21 mRNA levels are found to increase concomitantly with levels of NVP-CGM097 in tumor-bearing rats dosed at 30 mg/kg. The PD response is biphasic and prolonged up to 24 h. Additional p53 target genes such as MDM2 and PUMA mRNA levels are assessed in the tumor samples as well and showed a similar behavior. Daily treatment with NVP-CGM097 dose dependently and significantly inhibits SJSA-1 tumor growth in rats. It promotes stable disease at 20 mg/kg, which is associated with a plasma AUC0-24 of 163 μM•h. After iv administration, the total blood clearance (CL) of NVP-CGM097 is 5 mL/min per kg for mouse, 7 mL/min per kg for rat, 3 mL/min per kg for dog, and 4 mL/min per kg for monkey. The apparent terminal half-life (t1/2) is long in rodents and monkey (6-12 h) but is comparatively longer in dogs (20 h). After oral dosing, NVP-CGM097 is well absorbed with Tmax occurring between 1 and 4.5 h in all species tested. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.5169 mL | 7.5843 mL | 15.1685 mL | 30.3370 mL |
| 5mM | 0.3034 mL | 1.5169 mL | 3.0337 mL | 6.0674 mL |
| 10mM | 0.1517 mL | 0.7584 mL | 1.5169 mL | 3.0337 mL |
| 20mM | 0.0758 mL | 0.3792 mL | 0.7584 mL | 1.5169 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
+
%ddH2O
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Method for preparing DMSO master liquid:
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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