性能参数

产品名称

NVP-HDM201

规格

1mg 5mg 10mg 50mg 100mg

货号

GOY-Y3003

 含量

>98.00%

CAS

1448867-41-1

别名

N/A

化学名

N/A

分子式

C26H24Cl2N6O4

分子量

分子量 555.41

溶解度

DMSO : ≥ 56.75 mg/mL (102.18 mM)

储存条件

Store at -20°C

General tips

用途

仅供科研

价格

电询

详细内容

NVP-HDM201 (HDM201) is a potent and highly specific MDM-2/p53 inhibitor currently under phase I clinical trial.

NVP-HDM201 disrupts both human and murine TP53- MDM2 interactions, with nanomolar cellular IC50 values, blocking TP53 degradation[1].

NVP-HDM201 is an imidazolopyrrolidinone analogue, showing a very advantageous in vivo profile. NVP-HDM201 has recently entered Phase 1 clinical trials in cancer patients[2]. Constitutive PB mutagenesis in Arf-/- mice provides a collection of spontaneous tumors with characterized insertional genetic landscapes. Tumors are allografted in large cohorts of mice to assess the pharmacologic effects of NVP-HDM201. Sixteen out of 21 allograft models are sensitive to NVP-HDM201 but ultimately relapse under treatment. A comparison of tumors with acquired resistance to NVP-HDM201 and untreated tumors identified 87 genes that are differentially and significantly targeted by the PB transposon[1]. NVP-HDM201 administered either daily at a low dose or once at a high dose revealed a differentiated engagement of the p53 molecular response. In contrast to the daily low dose treatment regimen, the single high dose NVP-HDM201 regimen results in a rapid and dramatic induction of p53-dependent PUMA expression and apoptosis. This is consistent with the finding that a single high dose NVP-HDM201 treatment, administered orally or intravenously, results in a robust and sustained tumor regression. Overall, both daily and once every 3 weeks dosing regimen shows comparable long term efficacy in preclinical studies. The ongoing clinical trial is currently designed to compare both dosing regimens with regard to efficacy and tolerability[3].

壬基酚 GR  氟化铯 99.9% metals basis

对特辛基苯酚(POP)  97%  氟化铯 99%

4-甲基吡啶 98%  碘化铯 99.999%

1,5-戊二醇 97%  碘化铯 99.9%

丙酸酐 98%  氯化铯 SP

碘化钾  ACS, ≥99.0%  氯化铯 99.99% metals basis

RuBi-GABA10mg>98.00%Cas No. 1028141-88-9C42H39F6N5O2P2Ru

RuBi-4AP10mg>98.00%Cas No. 851956-02-0C30H28Cl2N8Ru

RuBi GABA trimethylphosphine10mg>98.00%Cas No.C27H33ClN5O2PRu

SCS50mg>98.00%Cas No. 3232-36-8C14H12N2O3

Sarcosine50mg>98.00%Cas No. 107-97-1C3H7NO2

ShK-Dap22100μg>98.00%Cas No. 220384-25-8C166H268N54O48S7

SN-650mg>98.00%Cas No. 415697-08-4C20H22N2O5S