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Purity: ≥98%
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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| References |
Proc Natl Acad Sci U S A.2017 Mar 21;114(12):3151-3156;Bioorg Med Chem Lett.2016 Oct 1;26(19):4837-4841.
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| Molecular Formula |
C26H24CL2N6O4
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| Molecular Weight |
555.41
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| Exact Mass |
| 554.1236 | |
| CAS # |
1448867-42-2
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| Related CAS # |
Siremadlin;1448867-41-1
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| SMILES |
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
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8005 mL | 9.0024 mL | 18.0047 mL | |
| 5 mM | 0.3601 mL | 1.8005 mL | 3.6009 mL | |
| 10 mM | 0.1800 mL | 0.9002 mL | 1.8005 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
Bcl-xL modulates the sensitivity of cell lines to TP53-MDM2 inhibition.Proc Natl Acad Sci U S A.2017 Mar 21;114(12):3151-3156. |
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Bcl-xL expression confers resistance to HDM201.Proc Natl Acad Sci U S A.2017 Mar 21;114(12):3151-3156. |
 Characterization of genetic modifications in HDM201-resistant tumors.Proc Natl Acad Sci U S A.2017 Mar 21;114(12):3151-3156. |
 Response and resistance to HDM201 TP53-MDM2 inhibitor allografted mice.Proc Natl Acad Sci U S A.2017 Mar 21;114(12):3151-3156. |
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 Characterization of response to HDM201 treatment of RosaPB/+;ATP2/+;Arf−/−allografted tumors.Proc Natl Acad Sci U S A.2017 Mar 21;114(12):3151-3156. |
 Resistance mechanisms identified in HDM201-resistant tumors.Representation of major PB transposon insertions found significantly enriched in RosaPB/+;ATP2/+;Arf−/−HDM201-resistant implanted tumors compared with untreated tumors (n= 95 tumors with differential PB insertions).Proc Natl Acad Sci U S A.2017 Mar 21;114(12):3151-3156. |
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