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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Cell Cycle > Abemaciclib MesylateCAS：1231930-82-7
Molecular Formula：C27H32F2N8·CH4O3S
Molecular Weight：602.7
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to yellow Solid
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| CAS | 1231930-82-7 |
| Name | Abemaciclib Mesylate |
| Molecular Formula | C27H32F2N8·CH4O3S |
| Molecular Weight | 602.7 |
| Solubility | Soluble in Water/DMSO |
| Purity | ≥98% |
| Appearance | White to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD25562906 |
| SMILES | CC(N1C2=CC(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)=CC(F)=C2N=C1C)C.CS(=O)(O)=O |
| Target Point | CDK4，CDK6 |
| Passage | Cell Cycle |
| Background | Abemaciclib Mesylate is a potent and selective inhibitor of CDK4 and CDK6. |
| Biological Activity | Abemaciclib (LY2835219) (methanesulfonate) 是选择性的 CDK4/6 抑制剂, 抑制 CDK4/CDK6 的 IC50 分别为 2 nM 和 10 nM[1-4]。 |
| IC50 | Cdk4/cyclin D1:2nM (IC50) CDK6/cyclinD1:10nM (IC50) CDK2/cyclinE:504nM (IC50) CDK9/cyclinT1:57nM (IC50) CDK1/cyclinB1:1627nM (IC50) CDK7/Mat1/cyclinH1:3910nM (IC50) Cdk5/p25:355nM (IC50) CDK5/p35:287nM (IC50) PIM1:50nM (IC50) PIM2:3400nM (IC50) HIPK2:31nM (IC50) DYRK2:61nM (IC50) CK2:117nM (IC50) GSK3b:192nM (IC50) JNK3:389nM (IC50) FLT3 (D835Y) :403nM (IC50) FLT3:3960nM (IC50) DRAK1:659nM (IC50) [1-4] |
| Data Literature Source | [1]. Ku BM， et al. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma. Oncotarget. 2016 Mar 22; 7 (12) :14803-13. [2]. Yadav V， et al. The CDK4/6 inhibitor LY2835219 overcomes vemurafenib resistance resulting from MAPK reactivation and cyclin D1 upregulation. Mol Cancer Ther. 2014 Oct; 13 (10) :2253-63. [3]. Gelbert LM， et al. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. Invest New Drugs. 2014 Oct; 32 (5) :825-37. [4]. Wu T， et al. Effect of abemaciclib (LY2835219) on enhancement of chemotherapeutic agents in ABCB1 and ABCG2 overexpressing cells in vitro and in vivo. Biochem Pharmacol. 2017 Jan 15; 124:29-42. |
| Unit | Bottle |
| Specification | 5mg 10mM*1mL in DMSO 10mg 20mg 50mg |
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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