您当前的位置：

Milciclib

(Synonyms: PHA-848125)

目录号: PL01494 纯度: ≥99%

Milciclib (PHA-848125) 是一种有效的、ATP 竞争性的 CDK 和 Tropomyosin receptor kinase (TRK) 双重抑制剂，对 cyclin A/CDK2，cyclin H/CDK7，cyclin D1/CDK4，cyclin E/CDK2，cyclin B/CDK1 和 TRKA 的 IC50 值分别为 45，150，160，363，398 和 53 nM。

CAS No. :802539-81-7

商品编号	规格	价格	会员价
PL01494-5mg	5mg	¥1525.00	请登录
PL01494-10mg	10mg	¥2255.00	请登录
PL01494-50mg	50mg	¥5485.00	请登录
PL01494-100mg	100mg	¥7465.00	请登录
PL01494-200mg	200mg	¥9865.00	请登录
PL01494-500mg	500mg	询价	询价
PL01494-10mM*1mLinDMSO	10mM*1mLinDMSO	¥3288.00	请登录
PL01494-1 mL x 10 mM (in DMSO)		¥1555.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

*注意事项:下单时请联系销售核实产品价格及货期，避免后续产生不便，感谢支持!

加入购物车在线咨询收藏产品大包装询价

中文名称	Milciclib
中文别名	4,5-二氢-n,1,4,4-四甲基-8-[[4-(4-甲基-1-哌嗪)苯基]氨基]-1H-吡唑并[4,3-h]喹唑啉-3-羧酰胺;4,5-二氢-N,1,4,4-四甲基-8-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-1H-吡唑并[4,3-H]喹唑啉-3-甲酰胺;PHA-848125 抑制剂;N,1,4,4-四甲基-8-((4-(4-甲基哌嗪-1-基)苯基)氨基)-4,5-二氢-1H-吡唑并[4,3-H]喹唑啉-3-甲酰胺
英文名称	Milciclib
英文别名	PHA-848125;Milciclib (PHA-848125);N,1,4,4-tetramethyl-8-[4-(4-methylpiperazin-1-yl)anilino]-5H-pyrazolo[4,3-h]quinazoline-3-carboxamide;Milciclib;PHA 848125;PHA848125;MMV676602;4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide;688000M8S8;N,1,4,4-tetramethyl-8-(4-(4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;Milciclib [INN];N,1,4,4-Tetramethyl-8-{[4-(4-Methylpiperazin-1-Yl)phenyl]amino}-4,5-Dihydro-1h-Pyrazolo[4,3-H]quinazoline-3-Carboxamide;N,1,4,4-tetr
Cas No.	802539-81-7
分子式	C₂₅H₃₂N₈O
分子量	460.57
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Milciclib (PHA-848125) 是一种有效的、ATP 竞争性的 CDK 和 Tropomyosin receptor kinase (TRK) 双重抑制剂，对 cyclin A/CDK2，cyclin H/CDK7，cyclin D1/CDK4，cyclin E/CDK2，cyclin B/CDK1 和 TRKA 的 IC50 值分别为 45，150，160，363，398 和 53 nM。

产品详情

Milciclib (PHA-848125) 是一种有效的、ATP 竞争性的 CDK 和 Tropomyosin receptor kinase (TRK) 双重抑制剂，对 cyclin A/CDK2，cyclin H/CDK7，cyclin D1/CDK4，cyclin E/CDK2，cyclin B/CDK1 和 TRKA 的 IC₅₀ 值分别为 45，150，160，363，398 和 53 nM。

生物活性

Milciclib (PHA-848125) is a potent, ATP-competitive and dual inhibitor of CDK and Tropomyosin receptor kinase (TRK), with IC 50 s of 45, 150, 160, 363, 398 nM and 53 nM for cyclin A/CDK2, cyclin H/CDK7, cyclin D1/CDK4, cyclin E/CDK2, cyclin B/CDK1 and TRKA, respectively.

性状

Solid

IC50 & Target[1][2]

cyclin A/CDK2 45 nM (IC50) cyclin E/CDK2 3

体外研究(In Vitro)

Milciclib (PHA-848125; 0.156 or 0.625 μM) up-regulates the expression of PDCD4, DDIT4, SESN2/sestrin 2 and DEPDC6/DEPTOR in GL-Mel cells. Milciclib (PHA-848125) potently inhibits the kinase activity of CDK2/cyclin A complex and of TRKA in a biochemical assay, with IC50s of 45 and 53 nM, respectively. Milciclib induces a clear accumulation of cells in G1 phase. Milciclib strongly inhibits NGF-induced phosphorylation of TRKA in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Milciclib (PHA-848125; 5, 10, and 15 mg/kg, p.o.) inhibits the growth of tumor in 7,12-dimethylbenz(a) anthracene (DMBA)-induced rat mammary carcinoma model. Milciclib has significant antitumor activity in various human xenografts and carcinogen-induced tumors as well as in disseminated primary leukemia models, with plasma concentrations in rodents in the same range as those found active in inhibiting cancer cell proliferation. Milciclib (PHA-848125; 40 mg/kg) induces a significant tumor growth inhibition in K-RasLA2 mice, and this is accompanied by a reduction in the cell membrane turnover. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Caporali S, Alvino E, Levati L, Esposito AI, Ciomei M, Brasca MG, Del Bufalo D, Desideri M, Bonmassar E, Pfeffer U, DAtri S. Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhib
[2]. Albanese C, Alzani R, Amboldi N, Avanzi N, Ballinari D, Brasca MG, Festuccia C, Fiorentini F, Locatelli G, Pastori W, Patton V, Roletto F, Colotta F, Galvani A, Isacchi A, Moll J, Pesenti E, Mercurio C, Ciomei M. Dual targeting of CDK and tropomyosin rec

溶解度数据	In Vitro: DMSO : 20 mg/mL (43.42 mM; Need ultrasonic)配制储备液

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Milciclib

相关产品

The molarity calculator equation

The dilution calculator equation