Abemaciclib - CAS 1231929-97-7

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BP-300081 100 mg $197 In stock
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Abemaciclib 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. It is used for the treatment of advanced or metastatic breast cancers.

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Molecular Formula
C27H32F2N8
Molecular Weight
506.61

Abemaciclib

    • Specification
      • Related CAS
        1231930-82-7 (mesylate)
        Purity
        ≥98%
        Appearance
        Light Yellow Solid
        IUPAC Name
        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
    • Properties
      • 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
    • Reference Reading
      • 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.
    • Preparing Stock Solutions
      • ConcentrationVolumeMass1 mg5 mg10 mg
        1 mM1.9740 mL9.8699 mL19.7398 mL
        5 mM0.3948 mL1.9740 mL3.9480 mL
        10 mM0.1974 mL0.9870 mL1.9740 mL
        50 mM---
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