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Rabusertib (LY2603618)

Cat. No. M2324
Rabusertib (LY2603618) Structure
Synonym:

Rabusertib ; IC-83

Size Price Availability Quantity
2mg USD 65  USD65 In stock
5mg USD 90  USD90 In stock
10mg USD 138  USD138 In stock
50mg USD 440  USD440 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Rabusertib (LY2603618) is an effective and selective Chk1 inhibitor with an IC50 of 7 nM.

Customer Product Validations & Biological Datas
Source Oncotarget (2017). Figure 2. LY2603618
Method Clonogenic survival
Cell Lines U2OS cells
Concentrations 0, 25, 50 or 100 nM
Incubation Time 24 hours
Results An exposure time of 24 hours to the inhibitors was chosen for the clonogenic survival assays to resemble a transient delivery of such inhibitors upon in vivo single injections.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 436.3
Formula C18H22BrN5O3
CAS Number 911222-45-2
Purity >98%
Solubility DMSO 12 mg/mL
Storage at -20°C
References

[1] Berta Laquente, et al. A phase II study to evaluate LY2603618 in combination with gemcitabine in pancreatic cancer patients

[2] Emiliano Calvo, et al. Phase I Study of CHK1 Inhibitor LY2603618 in Combination with Gemcitabine in Patients with Solid Tumors

[3] Darlene Barnard, et al. LY2603618, a selective CHK1 inhibitor, enhances the anti-tumor effect of gemcitabine in xenograft tumor models

[4] Enaksha R Wickremsinhe, et al. Disposition and metabolism of LY2603618, a Chk-1 inhibitor following intravenous administration in patients with advanced and/or metastatic solid tumors

[5] Constance King, et al. Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor

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  Catalog
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Keywords: Rabusertib (LY2603618), Rabusertib ; IC-83 supplier, Checkpoint, inhibitors

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