abemaciclib mesylate (LY2835219)

Name: abemaciclib mesylate (LY2835219)
Brand: Selleck Chemicals
SKU: S7158
Rating: 5 (28 reviews)

For research use only.

Catalog No.S7158

28 publications

abemaciclib mesylate (LY2835219) Chemical Structure

Molecular Weight(MW): 602.7

abemaciclib (LY2835219) is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.

Selleck's abemaciclib mesylate (LY2835219) has been cited by 28 publications

Cancer Discov, 2017, 7(10):1168-1183

PubMed: 28801307 ( click the link to review the publication )

Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Elife, 2020, 7;9:e44571

PubMed: 32255427 ( click the link to review the publication )

Haematologica, 2020, 2 pii: haematol

PubMed: 32241846 ( click the link to review the publication )

Cancers (Basel), 2020, 6;12(4)

PubMed: 32268485 ( click the link to review the publication )

Breast Cancer, 2020, 10.1007/s12282-020-01090-3

PubMed: 32297248 ( click the link to review the publication )

Mol Cell, 2019, 76(4):562-573

PubMed: 31543423 ( click the link to review the publication )

Nat Commun, 2019, 10(1):1373

PubMed: 30914635 ( click the link to review the publication )

Nat Commun, 2019, 10(1):557

PubMed: 30718506 ( click the link to review the publication )

Nat Commun, 2019, 10(1):558

PubMed: 30718512 ( click the link to review the publication )

Cancers (Basel), 2019, 11(2)

PubMed: 30736342 ( click the link to review the publication )

Mol Cancer Ther, 2019, 18(4):771-779

PubMed: 30837298 ( click the link to review the publication )

Mol Cancer Ther, 2019, 10.1158/1535-7163.MCT-19-0162

PubMed: 31395685 ( click the link to review the publication )

Cancer Biol Med, 2019, 16(2):264-275

PubMed: 31516747 ( click the link to review the publication )

J Oncol, 2019, 2019:5952836

PubMed: 31275382 ( click the link to review the publication )

Sci Immunol, 2019, 4(40)

PubMed: 31628160 ( click the link to review the publication )

Cancer Res, 2018, 78(15):4360-4369

PubMed: 29844123 ( click the link to review the publication )

Cell Death Dis, 2018, 9(10):944

PubMed: 30237504 ( click the link to review the publication )

Cell Death Dis, 2018, 9(9):918

PubMed: 30206211 ( click the link to review the publication )

Oncotarget, 2018, 9(45):27736-27751

PubMed: 29963233 ( click the link to review the publication )

Clin Cancer Res, 2017, 23(22):6946-6957

PubMed: 28830923 ( click the link to review the publication )

Dev Cell, 2017, 43(4):449-462

PubMed: 29103955 ( click the link to review the publication )

Int J Mol Sci, 2017, 18(10)

PubMed: 28961193 ( click the link to review the publication )

Oncotarget, 2017, 8(56):95116-95134

PubMed: 29221116 ( click the link to review the publication )
Oncotarget, 2017, 8(34):55848-55862

PubMed: 28915557 ( click the link to review the publication )

Nat Commun, 2016, 10.1038/ncomms10660

PubMed: 26876348 ( click the link to review the publication )

J Urol, 2015, 195(3):771-9

PubMed: 26318986 ( click the link to review the publication )

Biochem J, 2014, 459(3):513-24

PubMed: 24527759 ( click the link to review the publication )

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description

abemaciclib (LY2835219) is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM in cell-free assays, respectively. Phase 3.

Targets

CDK4 ^[1] (Cell-free assay)	CDK6 ^[1] (Cell-free assay)
2 nM	10 nM

In vitro

LY2835219 is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity. LY2835219 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of the serine/threonine kinases CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation. ^[1]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
insect cells	NGP2c4dHfW6ldHnvckBie3OjeR?=	M{nMNlUxKG2rboO=	M{LzfWNwdXCndHn0bZZmKGmwaHnibZRqd25ib3[gbJVu[W5iQ1TLOE9kgWOuaX6gSFEh\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhwenmuYYTpc44hd2ZiQ2TSSkBi\nSncjC1NEBucW6\|IHL5JG1q[2ijZXzpd{1O\W62ZX6gdIxwfCCjbnHsfZNqeyCrbjDwdoV{\W6lZTDv[kBCXFBuIFvpQVAvPiCwTR?=	NX7lOVBUOjZzMUW1O\|E>
insect cells	M2\zUWZ2dmO2aX;uJIF{e2G7	Mm\OOVAhdWmwcx?=	MXXJcohq[mm2aX;uJI9nKGi3bXHuJGNFUzRxY4njcIlvKERzIHX4dJJme3OnZDDpckBqdnOnY4SgZ4VtdHNiYYPz[ZN{\WRiYYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGNVWkZiYX\0[ZIhPTBibXnud{BjgSCvaXPyc5Bt[XSnIIPjbY51cWyuYYTpc44h[2:3boTldkwhUUN3ME2yJI5O	MWiyOlEyPTV5MR?=
human COLO205 cells	MVLGeY5kfGmxbjDhd5NigQ>?	Mn7uNlQhcA>?	NH;Lb2hKdmirYnn0bY9vKG:oIFPET\|QwPiCrbjDoeY1idiCFT1zPNlA2KGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25ib3[gVoIheGixc4Doc5J6dGG2aX;uJIFnfGW{IEK0JIhzeyCkeTDwdo9xcWSrdX2gbY9lcWSnIIP0ZYlvcW6pLXLhd4VlKGyjc3XyMZNk[W6waX7nJIZtfW:{ZYPj[Y5k\SCvaXPyc5Bt[XSnIHP5eI9u\XS{aXOgZY5idHm\|aYO=	MVmyOlEyPTV5MR?=
human COLO205 cells	M3fITmZ2dmO2aX;uJIF{e2G7	MXKyOEBp	NEjUUWdKdmirYnn0bY9vKG:oIFPET\|QwPiCrbjDoeY1idiCFT1zPNlA2KGOnbHzzJIF{e2W\|c3XkJIF{KG2jeHnteY0h[2WubDDjfYNt\SCjcoLld5Qh[XRiR{GgdIhie2ViYX\0[ZIhOjRiaILzJIJ6KHC{b4Dp[Il2dSCrb3Tp[IUhe3SjaX7pcocu[mG\|ZXSg[oxwfyCleYTvcYV1emmlIHHuZYx6e2m\|	M2\md\|I3OTF3NUex

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-Rb(S780) / Rb / p21; PubMed: 26909611 Oncotarget Effects of LY2835219 on RB phosphorylation and p21 expression were evaluated by immunoblotting at indicated concentrations (A) p-ERK / ERK / p-Akt / Akt / p-mTOR(S2448) / mTOR; PubMed: 26909611 Oncotarget Effects of LY2835219 on RB phosphorylation and p21 expression were evaluated by immunoblotting at indicated time points (B). pRb(S795) / E2F1 / Cyclin A2 / Cyclin E2; PubMed: 27748766 Oncogene (c) MCF-7 and MR cells were treated with 100 nm LY2835219 and collected at indicated times. Immunoblots were performed with the indicated antibodies. (d) MCF-7 and MR cells were treated with increasing concentrations of LY2835219 and harvested after 24 h; lysates were then subjected to immunoblotting.	26909611 27748766
Growth inhibition assay	Cell viability; PubMed: 26909611 Oncotarget Cell viability of OSC-19, FaDu, and YD-10B cells treated with LY2835219 at indicated concentrations. Data are representative of three independent experiments: mean ± SEM.	26909611

In vivo

LY2835219 saturates BBB efflux with an unbound plasma IC50 of about 95 nM. The percent of dose in brain for LY2835219-MsOH is 0.5–3.9%. In both a subcutaneous and intracranial human glioblastoma model (U87MG), LY2835219-MsOH suppressed tumor growth in a dose-dependent manner both as a single agent, and in combination with temozolomide. ^[1]

Protocol

References

[1] Corona SP, et al. Drug Des Devel Ther. 2018, 12:321-330.

Solubility (25°C)

In vitro	Water	100 mg/mL (165.92 mM)
	DMSO	83 mg/mL (137.71 mM)
	Ethanol	24 mg/mL (39.82 mM)
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): water For best results, use promptly after mixing.	100mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download abemaciclib mesylate (LY2835219) SDF

Molecular Weight	602.7
Formula	C₂₇H₃₂F₂N₈.CH₄O₃S
CAS No.	1231930-82-7
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A
Smiles	CCN1CCN(CC1)CC2=CC=C(NC3=NC(=C(F)C=N3)C4=CC(=C5N=C(C)[N](C(C)C)C5=C4)F)N=C2.C[S](O)(=O)=O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

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Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-05-15)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02327143	Completed	Drug: LY2835219\|Drug: ¹³C₈-LY2835219	Healthy Volunteers	Eli Lilly and Company	January 2015	Phase 1
NCT02256267	Completed	Drug: LY2835219\|Drug: Rifampin	Healthy Volunteers	Eli Lilly and Company	October 2014	Phase 1
NCT02059148	Completed	Drug: LY2835219	Healthy Volunteers	Eli Lilly and Company	February 2014	Phase 1
NCT02014129	Completed	Drug: LY2835219	Neoplasm Metastasis\|Lymphoma	Eli Lilly and Company	December 18 2013	Phase 1
NCT01913314	Completed	Drug: [^14C]-LY2835219	Healthy Volunteers	Eli Lilly and Company	August 2013	Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

Question 1:
Is your product S7158 LY2835219 “mesylate salt form”?
Answer:
Our S7158 LY2835219 is mesylate salt form.

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

Selective CDK Inhibitors

BS-181 HCl : CDK7-selective, IC50=21 nM.
Selective CDK Inhibitors

SNS-032 (BMS-387032) : CDK2-selective, IC50=48 nM.
CDK Inhibitor in Clinical Trial

Palbociclib (PD0332991) Isethionate : Phase III for Metastatic Breast Cancer.
Newest CDK Inhibitor

NU6027 : Potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with K_i of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.
Classic CDK Inhibitor

Palbociclib (PD-0332991) HCl : Highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 2/3.

Related CDK Products

SU9516 ^New

SU 9516 is a 3-substituted indolinone CDK inhibitor with IC50 of 22 nM, 40 nM, and 200 nM for CDK2, CDK1, and CDK4, respectively.
Ro-3306 ^New

RO-3306 is an ATP-competitive, and selective CDK1 inhibitor with K_i of 20 nM, >15-fold selectivity against a diverse panel of human kinases.
Purvalanol A ^New

Purvalanol A is a potent, and cell-permeable CDK inhibitor with IC50 of 4 nM, 70 nM, 35 nM, and 850 nM for cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, and cdk4-cyclin D1, respectively.
Palbociclib (PD-0332991) HCl

Palbociclib (PD-0332991) HCl is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays, respectively. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

Features:Non-cytotoxic, and halts cancer cell growth & could be used in glioblastoma that has relapsed after temozolomide treatment (a chemotherapeutic used to treat many cancers).
Palbociclib (PD0332991) Isethionate

Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM in cell-free assays. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

Features:The 1st specific inhibitor for CDK4/6 to show promise in multiple cancers.
Dinaciclib (SCH727965)

Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.
Flavopiridol HCl

Flavopiridol HCl competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.
Roscovitine (Seliciclib,CYC202)

Roscovitine (Seliciclib, CYC202) is a potent and selective CDK inhibitor for Cdc2, CDK2 and CDK5 with IC50 of 0.65 μM, 0.7 μM and 0.16 μM in cell-free assays. It shows little effect on CDK4/6. Phase 2.
Ribociclib (LEE011)

Ribociclib (LEE011) is an orally available, and highly specific CDK4/6 inhibitor. Phase 3.
SNS-032 (BMS-387032)

SNS-032 (BMS-387032) has firstly been described as a selective inhibitor of CDK2 with IC50 of 48 nM in cell-free assays and is 10- and 20-fold selective over CDK1/CDK4. It is also found to be sensitive to CDK7/9 with IC50 of 62 nM/4 nM, with little effect on CDK6. Phase 1.

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abemaciclib mesylate (LY2835219)