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Abemaciclib (LY2835219)

Cat. No. M10347

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Abemaciclib (LY2835219) Structure
Synonym:

LY2835219 free base

Size Price Availability Quantity
5mg USD 50  USD50 In stock
25mg USD 80  USD80 In stock
50mg USD 110  USD110 In stock
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Quality Control & Documentation
Biological Activity

Abemaciclib (LY2835219) is a best-in-class, selective and effective dual inhibitor of CDK4 and CDK6, which inhibits CDK4/CDK6 activity with IC50 of 2 nM and 10 nM respectively. LY2835219 is an orally effective cyclin-dependent kinase (CDK) inhibitor that targets CDK4 (Cyclin D1) and CDK6 (cyclin D3) cell cycle pathways and has potential antitumor activity. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting the phosphorylation of retinoblastoma (Rb) protein in the early G1 phase. Abemaciclib (LY2835219) inhibits Rb phosphorylation and prevents CDK-mediated G1-S phase transition, resulting in cell cycle stagnation in G1 phase, inhibiting DNA synthesis, and inhibiting cancer cell growth.


Chemical Information
Molecular Weight 506.59
Formula C27H32F2N8
CAS Number 1231929-97-7
Solubility (25°C) DMSO 3 mg/mL (ultrasonic and warming)
Storage 2-8°C, protect from light, sealed
References

[1] İbrahim Ethem Cakcak, et al. Turk J Med Sci. An experimental study: the effect of S. boulardii on abemaciclibinduced diarrhea

[2] Bo Mi Ku, et al. Oncotarget. The CDK4/6 inhibitor LY2835219 has potent activity in combination with mTOR inhibitor in head and neck squamous cell carcinoma

[3] Vipin Yadav, et al. Mol Cancer Ther. The CDK4/6 inhibitor LY2835219 overcomes vemurafenib resistance resulting from MAPK reactivation and cyclin D1 upregulation

[4] Lawrence M Gelbert, et al. Invest New Drugs. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine

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(E/Z)-Zotiraciclib citrate is a potent CDK2, JAK2, and FLT3 inhibitor.

Abemaciclib metabolites M2

Abemaciclib metabolite M2 (LSN2839567) is a metabolite of Abemaciclib, acts as a potent CDK4 and CDK6 inhibitor, with IC50 values of 1.2 and 1.3 nM, respectively.

CDK9-IN-1

CDK9-IN-1 is a novel, selective CDK9 inhibitor, with an IC50 of 39 nM for CDK9/CycT1, it can be used for the research of HIV infection.

XO44

XO44 (PF-6808472) is a broad-spectrum covalent kinase probe.

ML 315 

ML 315 is a selective dual inhibitor of CDK and DYRK with IC50s of 68 nM and 282 nM, respectively.

  Catalog
Abmole Inhibitor Catalog




Keywords: Abemaciclib (LY2835219), LY2835219 free base supplier, CDK, inhibitors, activators

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