MDX-1203
MDX-1203 (BMS-936561) is an antibody-drug conjugate targeting CD70. MDX-1203 binds to CD70 and mediates the specific delivery of its conjugated cytotoxic payload to tumors. MDX-1203 delivers a DNA alkylating payload into cells. MDX-1203 can be used in research related to advanced clear cell renal cell carcinoma and relapsed/refractory B-cell non-Hodgkin lymphoma.
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。
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
MDX-1203 binds CD70 with nanomolar affinity, induces dose-dependent cell death in CD70-expressing human tumor cell lines, and mediates antibody-dependent cellular cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC) following internalization[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MDX-1203 (10-100 mg/kg; i.v.; single dose, every 2 weeks; 3 doses) is safe at single 25 mg/kg and 100 mg/kg intravenous doses and repeated 10 mg/kg and 25 mg/kg intravenous doses every 2 weeks for 3 doses in Rattus norvegicus, but a single 50 mg/kg intravenous dose causes severe toxicity[2].
MDX-1203 (50 mg/kg; i.v.; repeated doses) is well tolerated in cynomolgus monkeys[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:unspecified strain[2]
-
Dosage:25 mg/kg (single i.v. dose); 100 mg/kg (single i.v. dose); 50 mg/kg (single i.v. dose); 10 mg/kg (i.v., every 2 weeks for 3 doses); 25 mg/kg (i.v., every 2 weeks for 3 doses)
-
Administration:i.v.; single dose; i.v.; every 2 weeks; 3 doses
-
Result:Were safe in single intravenous doses of 25 mg/kg and 100 mg/kg.
Resulted in severe toxicity (greater than 10% decrease in body weight compared to control animals) with a single 50 mg/kg intravenous dose.
Were safe with repeated intravenous doses of 10 mg/kg and 25 mg/kg (every 2 weeks for 3 doses).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
SMILES
[2H][M][X1203]
-
別名
BMS-936561
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
- MDX-1203
- BMS-936561
- MDX1203
- MDX 1203
- BMS936561
- BMS 936561
- Antibody-Drug Conjugates (ADCs)
- Transmembrane Glycoprotein
- clear cell renal cell carcinoma
- DNA alkylating payload
- rats
- B-cell non-Hodgkin lymphoma
- human tumor cell lines
- 786-O renal cell carcinoma xenograft model
- cynomolgus monkeys
- CDC
- CD70
- ADCC
- Inhibitor
- inhibitor
- inhibit