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| Size | Price | Stock |
|---|---|---|
| 2mg | $200 | 3-6 Days |
| 5mg | $360 | 3-6 Days |
| 10mg | $540 | 3-6 Days |
| 25mg | $910 | 3-6 Days |
| 50mg | $1300 | 3-6 Days |
| 100mg | $1880 | 3-6 Days |
| 250mg | $3180 | 3-6 Days |
: Cat #: V3167 CAS #: 1448867-42-2 Purity ≥ 98%
Description: HDM201 R Enantiomer is the R enantiomer of HDM201 (also called NVP-HDM201, HDM stands for 'human double minute 2 homolog'). HDM201 is an orally bioavailable, highly potent and selective inhibitor of the p53-Mdm2 protein-protein interaction. It has high affinity for Mdm2 in the picomolar range and a selectivity ratio of more than 10000-fold vs Mdm4. HDM201 is currently undergoing phase I clinical trial for cancer treatment. HDM201 inhibits the binding of the HDM2 protein to the transcriptional activation domain of the tumor suppressor protein p53. By preventing this HDM2-p53 protein-protein interaction, the proteosome-mediated enzymatic degradation of p53 is inhibited, which results in the restoration of both p53 signaling and p53-mediated induction of tumor cell apoptosis.
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| Molecular Weight (MW) | 555.41 |
|---|---|
| Molecular Formula | C26H24Cl2N6O4 |
| CAS No. | 1448867-42-2 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: ~100 mg/mL (180.0 mM) |
| Water: < 1 mg/mL | |
| Ethanol: 3 mg/mL (5.4 mM) | |
| SMILES Code | O=C1N(C2=CC(Cl)=CN(C)C2=O)[C@@H](C3=CC=C(Cl)C=C3)C4=C1N=C(C5=CN=C(OC)N=C5OC)N4C (C)C |
| Synonyms | HDM-201; HDM 201; HDM201; NVP-HDM 201; NVP-HDM201; NVP-HDM-201 |
| Protocol | In Vitro | In vitro activity: HDM201 acts by binding to the p53 binding-site of the Mdm2 protein, thereby disrupting the interaction of the two proteins (p53 and Mdm2) and leading to the activation of the p53 pathway. It induces robust p53-dependent cell cycle arrest and apoptosis in human p53 wild-type tumor cells. HDM201 exhibits highly selectivity across a panel of cancer cell lines Kinase Assay: Cell Assay: The in vitro combination screen was performed at Horizon Discovery (Cambridge, MA) on cancer cell lines, and data analysis was performed as described previously. Here we focused the data analysis on combinations with CGM097, a previous class of selective TP53-MDM2 inhibitors. A total of 485 cancer cell lines were treated with varying concentrations of CGM097 and for 25 other compounds. We integrated the information on TP53 mutation status and differentiated cell lines with no TP53 mutation from cell lines with TP53 alteration. We assessed the synergistic effect of combinations of HDM201and A-1155463 as described previously. |
|---|---|---|
| In Vivo | Treatment was initiated when the tumors engrafted in the flank were at least 150 mm3. Random enrollment was applied. Efficacy studies, tumor response, and relapse were reported with the measures of tumor volumes at the start of treatment. HDM201 was administered at 100 mg/kg in 0.5% methylcellulose and 0.1% Tween 80 orally twice a week, with alternating intervals of 3 d and 4 d. Vehicle was generated according to the formulation. Treatments were administered in the morning. | |
| Animal model | Mouse |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.8005 mL | 9.0024 mL | 18.0047 mL | 36.0094 mL |
| 5mM | 0.3601 mL | 1.8005 mL | 3.6009 mL | 7.2019 mL |
| 10mM | 0.1800 mL | 0.9002 mL | 1.8005 mL | 3.6009 mL |
| 20mM | 0.0900 mL | 0.4501 mL | 0.9002 mL | 1.8005 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.
- (2) Be sure to add the solvent(s) in order.