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Prexasertib dihydrochloride
CAS No. 1234015-54-3
Prexasertib dihydrochloride( LY-2606368 dihydrochloride | LY 2606368 dihydrochloride )
Catalog No. M10929 CAS No. 1234015-54-3
A potent, selective, ATP-competitive inhibitor of CHK1 with Ki of 0.9 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 88 | In Stock |
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| 2MG | 51 | In Stock |
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| 5MG | 85 | In Stock |
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| 10MG | 140 | In Stock |
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| 25MG | 274 | In Stock |
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| 50MG | 419 | In Stock |
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| 100MG | 617 | In Stock |
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| 200MG | Get Quote | In Stock |
|
| 500MG | 1293 | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NamePrexasertib dihydrochloride
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective, ATP-competitive inhibitor of CHK1 with Ki of 0.9 nM.
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DescriptionA potent, selective, ATP-competitive inhibitor of CHK1 with Ki of 0.9 nM; potently abrogates the G2-M checkpoint activated by doxorubicin in p53-deficient HeLa cells with EC50 of 9 nM; causes replication catastrophe in vitro and in vivo; shows significant tumor growth inhibition in xenograft tumor models.Lung Cancer Phase 2 Clinical.
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In VitroCell Cycle AnalysisCell Line:HeLa cells Concentration:33, 100 nM.Incubation Time:For 7 hours Result:Had an IC50 of 37 nM and resulted in the G2-M population received DNA damage during S-phase but continued to progress through the cell cycle into an early mitosis.Western Blot Analysis Cell Line:HT-29 cells.Concentration:8, 16, 31, 63, 125, 250 nM.Incubation Time:Pre-treated for 15 minutes Result:Inhibited CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) (IC50 of less than 31 nM) in HT-29 cells.
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In VivoAnimal Model:Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cellsDosage:1, 3.3, or 10 mg/kg Administration:SC; twice daily for 3 days, rest 4 days; for three cyclesResult:Caused statistically significant tumor growth inhibition (up to 72.3%).Animal Model:Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells Dosage:15 mg/kg (Pharmacokinetic Analysis) Administration:SC (200 μL) Result:CHK1 was 7 ng/mL at 12 hours and 3 ng/mL by 24 hours in plasma exposures. Phosphorylation of both H2AX (S139) and RPA2 (S4/S8) was detectable at 4 hours, showing the rapid occurrence of DNA damage.
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SynonymsLY-2606368 dihydrochloride | LY 2606368 dihydrochloride
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PathwayAngiogenesis
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TargetChk
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RecptorChk1|Chk2|RSK
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Research AreaCancer
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IndicationLung Cancer
Chemical Information
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CAS Number1234015-54-3
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Formula Weight438.311
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Molecular FormulaC18H21Cl2N7O2
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 32 mg/mL
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SMILESCOC1=C(C(=CC=C1)OCCCN)C2=CC(=NN2)NC3=NC=C(N=C3)C#N.Cl.Cl
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Chemical Name2-Pyrazinecarbonitrile, 5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]-, hydrochloride (1:2)
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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SB-218078
A potent inhibitor of Chk1 that blocks phosphorylation of cdc25 with IC50 of 15 nM.
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SAR-020106
SAR-020106 is a potent, ATP-competitive, and selective CHK1 inhibitor with an IC50 of 13.3 nmol/L on the isolated human enzyme.SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC(50) of 13.3 nmol/L on the isolated human enzyme. This compound abrogates an etoposide-induced G(2) arrest with an IC(50) of 55 nmol/L in HT29 cells, and significantly enhances the cell killing of gemcitabine and SN38 by 3.0- to 29-fold in several colon tumor lines in vitro and in a p53-dependent fashion.
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CCT-245737
A highly potent, selective, ATP-competitive inhibitor of Chk1 with IC50 of 1.3 nM; weak inhibition on Chk2 (IC50=2440 nM).
