423148-78-1
- CAS号:423148-78-1
- 英文名:(E)-1-(3-chloro-4-fluorophenyl)-4-((5-nitrofuran-2-yl)Methylene)pyrazolidine-3,5-dione
- 中文名:423148-78-1
- CBNumber:CB82609290
- 分子式:C14H7ClFN3O5
- 分子量:351.67
- MOL File:423148-78-1.mol
- 密度 :1.662±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 形态 :solid
- 酸度系数(pKa) :7.12±0.20(Predicted)
- 颜色 :Brown
423148-78-1性质、用途与生产工艺
- 生物活性 PYZD-4409 是 ubiquitin-activating enzyme UBA1 的特异性抑制剂，其 IC50 值为 20 μM。PYZD-4409 能诱导恶性细胞死亡，并优先抑制原发性急性髓性白血病细胞的生长。
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靶点
IC50: 20 μM (ubiquitin-activating enzyme UBA1)
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体外研究
PYZD-4409 (10-40 μM; 72 hours; myeloma, leukemia, and solid tumor cell lines, primary AML cells and normal hematopoietic cells) induces cell death with a LD 50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. In contrast, solid tumor cell lines were less sensitive with an LD 50 of approximately 15 to 20 μM. PYZD-4409 is preferentially cytotoxic to malignant cells over normal hematopoietic cells.
PYZD-4409 (50 μM; 4 hours; K562 leukemia cells) treatment blocks the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34.
PYZD-4409 (0-25 μM; 24 hours; K562 leukemia cells) significantly increases both mRNA and protein levels of Grp78 and Hsp70. In addition, PYZD-4409 increases levels of phospho-JNK and phospho-p38 mitogen-activated protein kinase, which have also been linked to ER stress and the unfolded protein response.Cell Cytotoxicity Assay
Cell Line: Myeloma, leukemia, and solid tumor cell lines, primary AML cells and normal hematopoietic cells Concentration: 10 μM, 20 μM, 30 μM, 40 μM Incubation Time: 72 hours Result: Induced cell death with a LD 50 less than 10 μM in 5 of 8 leukemia and myeloma cell lines. In contrast, solid tumor cell lines were less sensitive with an LD 50 of approximately 15 to 20 μM. Western Blot Analysis
Cell Line: K562 leukemia cells Concentration: 50 μM Incubation Time: 4 hours Result: Blocked the E1-dependent conjugation of ubiquitin to the E2 enzyme cdc34. RT-PCR
Cell Line: K562 cells Concentration: 0 μM, 10 μM, 25 μM Incubation Time: 24 hours Result: Significantly increased both mRNA and protein levels of Grp78 and Hsp70. -
体内研究
PYZD-4409 (10 mg/kg; intraperitoneal injection; daily on alternate days; for 16 days; male severe combined immunodeficient mice) decreases tumor weight and volume without untoward toxicity.
Animal Model: Male severe combined immunodeficient (SCID) mice with MDAY-D2 murine leukemia cells Dosage: 10 mg/kg Administration: Intraperitoneal injection; daily on alternate days; for 16 days Result: Delayed tumor growth and decreased tumor weight without untoward toxicity.
- 更新日期：2024/11/08
- 产品编号：HY-13297
- 产品名称：PYZD-4409
- CAS编号：
- 包装：1 mg
- 价格：750元
- 更新日期：2024/11/08
- 产品编号：HY-13297
- 产品名称：423148-78-1 PYZD-4409
- CAS编号：423148-78-1
- 包装：5mg
- 价格：1800元
- 公司名称：Musechem
- 联系电话：+1-800-259-7612
- 电子邮件：info@musechem.com
- 国家：美国
- 产品数：4660
- 优势度：60
- 公司名称：TargetMol Chemicals Inc.
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- 电子邮件：marketing@targetmol.com
- 国家：美国
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- 公司名称：Aladdin Scientific
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