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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Cell Cycle > MilciclibCAS：802539-81-7
Molecular Formula：C25H32N8O
Molecular Weight：460.57
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to yellow Solid
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| CAS | 802539-81-7 |
| Name | Milciclib |
| Molecular Formula | C25H32N8O |
| Molecular Weight | 460.57 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD17169990 |
| SMILES | O=C(NC)C1=NN(C2=C1C(C)(CC3=CN=C(N=C23)NC4=CC=C(C=C4)N5CCN(CC5)C)C)C |
| Target Point | CDK;TrkA |
| Passage | Cell Cycle;Protein Tyrosine Kinase/RTK;Neuronal Signaling |
| Background | Milciclib is a potent dual inhibitor of CDK and Tropomyosin receptor kinase (TRK). |
| Biological Activity | Milciclib 是一种有效的 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。[1-3] |
| IC50 | cyclin A/CDK2:45nM;cyclin E/CDK2:363nM [1-3] |
| Data Literature Source | [1]. Caporali S，Alvino E，Levati L，Esposito AI，Ciomei M，Brasca MG，Del Bufalo D，Desideri M，Bonmassar E，Pfeffer U，D'Atri S.Down-regulation of the PTTG1 proto-oncogene contributes to the melanoma suppressive effects of the cyclin-dependent kinase inhibitor PHA-848125.Biochem Pharmacol. 2012 Sep 1;84(5):598-611. [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 receptor kinase families by the oral inhibitor PHA-848125，an agent with broad-spectrum antitumor efficacy.Mol Cancer Ther. 2010 Aug;9(8):2243-54. [3]. Degrassi A，et al. Efficacy of PHA-848125，a cyclin-dependent kinase inhibitor，on the K-Ras(G12D)LA2 lung adenocarcinoma transgenic mouse model: evaluation by multimodality imaging.Mol Cancer Ther. 2010 Mar;9(3):673-81 |
| Unit | Bottle |
| Specification | 5mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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