Abemaciclib ( LY2835219)
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 205911

CAS#: 1231929-97-7 (free base)

Description: Abemaciclib, also known as LY2835219, is 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 inhibits CDK4 and CDK6 with low nanomolar potency. 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.


Price and Availability

Size
Price

25mg
USD 90
200mg
USD 350
2g
USD 1250
20g
USD 5650
Size
Price

50mg
USD 150
500mg
USD 550
5g
USD 2450
50g
Ask price
Size
Price

100mg
USD 250
1g
USD 750
10g
USD 3850

Abemaciclib (LY2835219) free base purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 2g may be 2 weeks.


Chemical Structure

img

Theoretical Analysis

MedKoo Cat#: 205911
Name: Abemaciclib ( LY2835219)
CAS#: 1231929-97-7 (free base)
Chemical Formula: C27H32F2N8
Exact Mass: 506.2718
Molecular Weight: 506.59339
Elemental Analysis: C, 64.01; H, 6.37; F, 7.50; N, 22.12


Synonym: LY2835219; LY2835219; LY 2835219; Abemaciclib.

IUPAC/Chemical Name: N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl)-5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazol-6-yl)pyrimidin-2-amine

InChi Key: UZWDCWONPYILKI-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: CC1=NC2=C(F)C=C(C3=NC(NC4=NC=C(CN5CCN(CC)CC5)C=C4)=NC=C3F)C=C2N1C(C)C


Technical Data

Appearance:
White to offer white solid

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0-4 C for short term (weeks), and -20 C for long term (months)

Harmonized System Code:
293490


Additional Information

Related CAS#
CAS#1231929-97-7 (LY2835219 free base)
CAS# 1231930-82-7 (LY2835219 mesylate salt).


References

1: Yadav V, Burke TF, Huber L, Van Horn RD, Zhang Y, Buchanan SG, Chan EM, Starling JJ, Beckmann RP, Peng SB. The CDK4/6 Inhibitor LY2835219 Overcomes Vemurafenib Resistance Resulting from MAPK Reactivation and Cyclin D1 Upregulation. Mol Cancer Ther. 2014 Aug 13. pii: molcanther.0257.2014. [Epub ahead of print] PubMed PMID: 25122067.

2: Gelbert LM, Cai S, Lin X, Sanchez-Martinez C, Del Prado M, Lallena MJ, Torres R, Ajamie RT, Wishart GN, Flack RS, Neubauer BL, Young J, Chan EM, Iversen P, Cronier D, Kreklau E, de Dios A. 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 Jun 13. [Epub ahead of print] PubMed PMID: 24919854.

3: Tate SC, Cai S, Ajamie RT, Burke T, Beckmann RP, Chan EM, De Dios A, Wishart GN, Gelbert LM, Cronier DM. Semi-mechanistic pharmacokinetic/pharmacodynamic modeling of the antitumor activity of LY2835219, a new cyclin-dependent kinase 4/6 inhibitor, in mice bearing human tumor xenografts. Clin Cancer Res. 2014 Jul 15;20(14):3763-74. doi: 10.1158/1078-0432.CCR-13-2846. Epub 2014 May 21. PubMed PMID: 24850847.

4: Dickson MA. Molecular pathways: CDK4 inhibitors for cancer therapy. Clin Cancer Res. 2014 Jul 1;20(13):3379-83. doi: 10.1158/1078-0432.CCR-13-1551. Epub 2014 May 2. PubMed PMID: 24795392.