LY3143921( LY-3143921 | LY 3143921 )

Catalog No. M12416 CAS No. 1627696-53-0

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

LY3143921
Note

Research use only, not for human use.
Brief Description

LY3143921 (LY-3143921) is an orally available, potent, selective inhibitor of Cdc7 kinase inhibitor, inhibits CDC7/DBF4 I and pMCM2 (S53) with IC50 values of 3.3 nM and 290 nM, respectively.
Description

LY3143921 (LY-3143921) is an orally available, potent, selective inhibitor of Cdc7 kinase inhibitor, inhibits CDC7/DBF4 I and pMCM2 (S53) with IC50 values of 3.3 nM and 290 nM, respectively.Solid Tumors Phase 1 Clinical.
In Vitro

LY3177833 (10 μM; 4 days) increases SA-β-gal content in Hep3B cells.Western Blot Analysis Cell Line:Hep3B cells Concentration:10 μM Incubation Time:4 days Result:Increased the expression of human SA-β-gal.
In Vivo

LY3177833 (Example 4; 10.4-31.2 mg/kg; oral gavage; twice a day; for 2 weeks; female athymic Balb/c nude mice with SW620 cells) treatment causes significant tumor regression in a dose-dependent manner. Also, no significant tumor growth is observed for 2 weeks after dosing cessation. Animal Model:Female athymic Balb/c nude mice (5-6 weeks old) with SW620 cellsDosage:10.4 mg/kg, 20.8 mg/kg and 31.2 mg/kg Administration:Oral gavage; twice a day for 2 weeksResult:Showed dose dependent antitumor activity in SW620 mouse xenograft tumor model.
Synonyms

LY-3143921 | LY 3143921
Pathway

Cell Cycle/DNA Damage
Target

CDK
Recptor

CDK
Research Area

Cancer
Indication

Solid Tumors

CAS Number

1627696-53-0
Formula Weight

327.319
Molecular Formula

C16H14FN5O2
Purity

>98% (HPLC)
Solubility

——
SMILES

CC1(C2=C(C=C(C=C2)C3=CNN=C3)C(=O)N1)C4=NC=NC=C4F.O
Chemical Name

(3R)-3-(5-Fluoro-4-pyrimidinyl)-2,3-dihydro-3-methyl-6-(1H-pyrazol-4-yl)-1H-isoindol-1-one hydrate