PIM-447 (dihydrochloride)

中文名	PIM-447 (dihydrochloride)
英文名	PIM-447 (dihydrochloride)
别名	泛PIM抑制剂化合物 T12473
英文别名	EOS-62253 PIM-447 2HCl PIM447 DIHYDROCHLORIDE LGH-447 dihydrochloride PIM-447 (dihydrochloride) N-(4-((1R,3S,5S)-3-amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide
CAS	1820565-69-2
化学式	C24H23F3N4O
分子量	440.4608296
溶解度	DMSO: ≥ 46.7 mg/mL
存储条件	-20℃
体外研究	PIM-447(0.05-10 µM; 24, 48 and 72 hours)has inhibitory effects in MM cells, it against sensitive cell lines with IC 50 values ranging from 0.2 to 3.3 µM (MM1S, MM1R, RPMI-8226, MM144, U266 and NCI-H929) and less sensitive cell lines with IC 50 values at 48 h >7 µM (OPM-2,RPMI-LR5, U266-Dox4 and U266-LR7).PIM-447(0.1-10 µM; 24, 48 and 72 hours) does not induce important levels of apoptosis, when PIM447 at 5 µM, it substantially increases annexin-V levels (about 30%) in sensitive cell lines(MM1S, NCI-H929 and RPMI-8226).when PIM447 at 10 µM, it induces apoptosis in all the cell lines but to a lesser extent in OPM-2 and RPMI-LR5.PIM447 promotes the cleavage of initiator caspases, such as caspases 8 and 9, and increases the cleavage of the effector caspases 3 and 7, together with PARP cleavage in MM1S,RPMI-8226 and NCI-H929 cells.PIM447 (0.1-1 µM) increases the percentage of cells in the G0/G1 phase and decreases the proliferative phases (S and G2/M) of the cell cycle. The effects at low concentrations (0.1-1 µM) were more pronounced in MM1S cells than in OPM-2. Cell Viability Assay Cell Line: Sensitive MM cell lines: MM1S, MM1R, RPMI-8226, MM144, U266 and NCI-H929 cells Less sensitive MM cell lines: OPM-2,RPMI-LR5, U266-Dox4 and U266-LR7cells Concentration: 0.05-10 µM Incubation Time: 24, 48 and 72 hours Result: Was cytotoxic for MM cells (PIM kinases highly expressed). Apoptosis Analysis Cell Line: Sensitive MM cell lines: MM1S, NCI-H929 and RPMI-8226 cells Less sensitive MM cell lines: OPM-2 and RPMI-LR5 cells Concentration: 0.05-10 µM Incubation Time: 24, 48 and 72 hours Result: Induced cell apoptosis at higer doses, had no effects at 0.1-1 uM. Western Blot Analysis Cell Line: Sensitive MM cell lines: MM1S, NCI-H929 and RPMI-8226 cells Concentration: 0.05-10 µM Incubation Time: 24, 48 hours Result: Increased the cleavage of the effector caspases 3 and 7, and the PARP cleavage. Cell Cycle Analysis Cell Line: MM1S, OPM-2 cells Concentration: 0.1, 0.5 or 1 µM Incubation Time: 48 hours Result: Increased the cleavage of the effector caspases 3 and 7, and the PARP cleavage.
体内研究	PIM447 (oral gavage; 100 mg/kg; 5 times/week) clearly controlls tumor progression and the serum levels of hIgλ secreted by RPMI-8226-luc cells in mouse model of bone marrow-disseminated human multiple myeloma. Animal Model: RPMI-8226-luc cells are injected intravenously into 6-week-old female NODSCID-IL-2Rγ -/- (NSG) mice Dosage: 100 mg/kg Administration: oral gavage; 100 mg/kg; 5 times/week Result: Was well tolerated, as the body weight of mice did not decrease by more than 10%. Increased bone volume density and trabecular number and reduced trabecular separation relative to vehicle group.

PIM-447 (dihydrochloride) - 配置溶液浓度参考

	1mg	5mg	10mg
1 mM	1.948 ml	9.739 ml	19.479 ml
5 mM	0.39 ml	1.948 ml	3.896 ml
10 mM	0.195 ml	0.974 ml	1.948 ml
5 mM	0.039 ml	0.195 ml	0.39 ml

最后更新：2024-01-02 23:10:35

PIM-447 (dihydrochloride) - 简介

PIM-447 (dihydrochloride) 是一种化合物，其化学名称为PIM-447二盐酸盐。PIM-447是一种选择性的PIM激酶抑制剂。

PIM-447有着广泛的用途。实验证明PIM-447能够抑制肿瘤细胞的生长和扩散，增强化疗的疗效，并减少耐药性。

制备PIM-447 (dihydrochloride) 的方法是通过化学合成。具体的制备方法可以通过文献或专利进行查询。
如需使用该化合物，请遵循化学物品的正确处理和储存方法，并按照相关安全指南进行操作。

最后更新：2024-04-09 19:05:04

MedChemExpress

现货供应

产品名: PIM-447 去供应商网站查看询盘
CAS: 1820565-69-2
产地: 美国
包装: 10 mM * 1 mL;10 mM * 1 mL;1 mg;1 mg;5 mg;5 mg;10 mg;10 mg
规格: HY-19322B
库存: 现货，货期：1-2天
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产品描述: 产品覆盖：8万多种抑制剂，11000+靶点蛋白，数百款试剂盒，200+生物活性化合物库，天然产物，抗体等. 纯度: 99.94%

上海吉至生化科技有限公司

现货供应

产品名: PIM447 DIHYDROCHLORIDE 去供应商网站查看询盘
CAS: 1820565-69-2
产地: 中国上海
包装: 1mg，50mg，10mg，5mg，100mg
价格: 面议、电联、微信、QQ
库存: 现货
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产品描述: 中文名称：PIM447 DIHYDROCHLORIDE ，英文名称：PIM-447 dihydrochloride，CAS：1820565-69-2 ，包装：1 更多

上海麦克林生化科技股份有限公司

现货供应

产品名: PIM-447 dihydrochloride 去供应商网站查看询盘
CAS: 1820565-69-2
产地: 上海
规格: P881167
价格: 1mg-1216,5mg-3647
库存: 7天内发货
电话: 13816333479/17821173903
手机: 13816333479/17821173903
电子邮件: wangrui@macklin.cn
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上海源叶生物科技有限公司

产品名: PIM-447 (dihydrochloride) 去供应商网站查看询盘
CAS: 1820565-69-2
产地: 上海
规格: 99%
价格: 1mg 1000,5mg 3000,10mg 5000
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