MIP-1095
MIP-1095 (RPS-001) is a PSMA inhibitor with a Ki value of 0.24 nM. MIP-1095 binds to PSMA with high affinity and can be internalized into PSMA-expressing cancer cells. When radiolabeled with 123I, 124I or 131I, MIP-1095 enables SPECT/CT imaging, PET/CT imaging or targeted radiation delivery, respectively. 131I-MIP-1095 can alter serum PSA levels and relieve bone pain. MIP-1095 can be used in research related to metastatic castration-resistant prostate cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 949575-22-8
- 分子式: C19H25IN4O8
- 分子量:564.33
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Radionuclide-Drug Conjugates (RDCs) アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
10 nM
Compound: 20
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Inhibition of [131I]DCIT from PSMA in human LNCAP cells
Inhibition of [131I]DCIT from PSMA in human LNCAP cells
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[PMID: 19111054] |
体外実験
MIP-1095 (1-10000 nM; 30 minutes) potently inhibits the NAALADase activity of PSMA in human prostate cancer LNCaP cell lysates with a Ki of 0.24 nM[1].
[123I]MIP-1095 (3 nM; 1 hour) binds specifically to PSMA-positive human prostate cancer LNCaP cells but not to PSMA-negative human prostate cancer PC3 cells, with binding blocked by non-radiolabeled MIP-1095 or PMPA[1].
[123I]MIP-1095 (100 nM; 0-2 hour) undergoes time- and temperature-dependent internalization into human prostate cancer LNCaP cells via endocytosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Fox Chase SCID (male)[1]
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Dosage:1 mCi/mouse
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Administration:i.v. tail vein
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Result:Showed high, selective uptake in PSMA-expressing tissues: LNCaP tumors and kidneys at 4 hours post-injection.
Detected PC3 PIP (PSMA+) tumors but not PC3 flu (PSMA-) tumors at 2 hours post-injection.
化学情報
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CAS 番号 949575-22-8
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分子量 564.33
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分子式 C19H25IN4O8
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SMILES
O=C(O)CC[C@@H](C(O)=O)NC(N[C@H](C(O)=O)CCCCNC(NC1=CC=C(I)C=C1)=O)=O
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別名
RPS-001
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[1]. Hillier SM, et al. Preclinical evaluation of novel glutamate-urea-lysine analogues that target prostate-specific membrane antigen as molecular imaging pharmaceuticals for prostate cancer. Cancer research. 2009 Sep 01;69(17):6932-40. [Content Brief]
[2]. Zechmann CM, et al. Radiation dosimetry and first therapy results with a (124)I/ (131)I-labeled small molecule (MIP-1095) targeting PSMA for prostate cancer therapy. European journal of nuclear medicine and molecular imaging. 2014 Jul;41(7):1280-92. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
MIP-1095 関連分類
HY-123733 関連分類
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