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Longdaysin

Cat. No. M10107
Longdaysin Structure
Size Price Availability Quantity
5mg USD 90  USD90 In stock
10mg USD 140  USD140 In stock
25mg USD 280  USD280 In stock
50mg USD 450  USD450 In stock
100mg USD 660  USD660 In stock
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Quality Control & Documentation
Biological Activity

Longdaysin is a Casein Kinase inhibitor with IC50 values of 8.8 μM, 5.6 μM, 52 μM and 29 μM for CKIδ, CKIα, ERK2 and CDK7. In breast cancer Hs578T and MDA-MB-231 cells, micromolar concentrations of longdaysin attenuated the phosphorylation of LRP6 and DVL2 and reduced the expression of active β-catenin and total β-catenin, leading to the downregulation of Wnt target genes Axin2, DKK1, LEF1, and Survivin. In MDA-MB-231 breast cancer xenografts, treatment with longdaysin suppressed tumor growth in association with inhibition of Wnt/β-catenin signaling.

Chemical Information
Molecular Weight 335.33
Formula C16H16F3N5
CAS Number 1353867-91-0
Solubility (25°C) DMSO ≥ 70 mg/mL
Storage 2-8°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yanpeng Xiong, et al. Onco Targets Ther. Longdaysin inhibits Wnt/β-catenin signaling and exhibits antitumor activity against breast cancer

[2] Tsuyoshi Hirota, et al. PLoS Biol. High-throughput chemical screen identifies a novel potent modulator of cellular circadian rhythms and reveals CKIα as a clock regulatory kinase

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Keywords: Longdaysin supplier, Casein Kinase, inhibitors, activators


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