Name: Abemaciclib
Brand: BOC Sciences
Price: 197 USD
Availability: MadeToOrder

Size

Price

Stock

Quantity

100 mg

$197

In stock

Purity

≥98%

Appearance

Light Yellow Solid

IUPACName

N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine

Synonyms

LY-2835219; LY 2835219; LY2835219; Verzenio; N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-2-amine

Melting Point

175-178°C

InChI Key

UZWDCWONPYILKI-UHFFFAOYSA-N

InChI

InChI=1S/C27H32F2N8/c1-5-35-8-10-36(11-9-35)16-19-6-7-24(30-14-19)33-27-31-15-22(29)25(34-27)20-12-21(28)26-23(13-20)37(17(2)3)18(4)32-26/h6-7,12-15,17H,5,8-11,16H2,1-4H3,(H,30,31,33,34)

Canonical SMILES

CCN1CCN(CC1)CC2=CN=C(C=C2)NC3=NC=C(C(=N3)C4=CC5=C(C(=C4)F)N=C(N5C(C)C)C)F

1.Optimising the combination dosing strategy of abemaciclib and vemurafenib in BRAF-mutated melanoma xenograft tumours.

Tate SC1, Burke TF2, Hartman D2, Kulanthaivel P2, Beckmann RP2, Cronier DM1. Br J Cancer. 2016 Mar 15;114(6):669-79. doi: 10.1038/bjc.2016.40.

BACKGROUND: Resistance to BRAF inhibition is a major cause of treatment failure for BRAF-mutated metastatic melanoma patients. Abemaciclib, a cyclin-dependent kinase 4 and 6 inhibitor, overcomes this resistance in xenograft tumours and offers a promising drug combination. The present work aims to characterise the quantitative pharmacology of the abemaciclib/vemurafenib combination using a semimechanistic pharmacokinetic/pharmacodynamic modelling approach and to identify an optimum dosing regimen for potential clinical evaluation.

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	1.9740 mL	9.8699 mL	19.7398 mL
5 mM	0.3948 mL	1.9740 mL	3.9480 mL
10 mM	0.1974 mL	0.9870 mL	1.9740 mL
50 mM	-	-	-

Since we want to administer Abemaciclib to mice for the relevant experiments, what is the appropriate way to administer it to mice ?

Abemaciclib can be dissolved in 1% HEC in 20 mM phosphate buffer (pH 2.0) and administered to mice by oral tube feeding.

9/4/2018

We wondered if the use of Abemaciclib on HNSCC cells would have an effect on the mTOR pathway ?

Abemaciclib decreased cell viability and inhibited Akt and ERK signaling but not mTOR activation in head and neck squamous cell carcinoma (HNSCC) cells.

11/5/2019

As a selective CDK4/6 inhibitor, what is the specific IC50 for Abemaciclib ?

Abemaciclib inhibits CDK4/CDK6 activity with IC50s of 2 nM and 10 nM, respectively.

27/11/2021

stimulation of PIM

We used purchased Abemaciclib as a stimulation of PIM targets, but it turned out that it acted on PIM1 with an IC50 of 50 nM, whereas it acted on PIM2 with an IC50 of 3,400 nM. The difference was quite significant.

22/10/2018

specific for Rb-skilled cells

Abemaciclib could inhibit CDK4 and CDK6 with low nanomolar potency, inhibiting Rb phosphorylation, leading to G1 arrest and inhibition of proliferation, which is consistent with the literature results. However, we found that Abemaciclib was inhibiting Rb phosphorylation and its activity was specific for Rb-skilled cells, which deserves further exploration.

9/8/2019

reduce cell viability

Abemaciclib has a potent ability to reduce cell viability! Its IC50 values range from 0.5 μM to 0.7 μM.

25/2/2023

Stock concentration: *

Desired final volume: *

Desired concentration: *

* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂