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NSC 617145

Cat. No. M11056
NSC 617145 Structure
Size Price Availability Quantity
5mg USD 85  USD85 In stock
10mg USD 125  USD125 In stock
25mg USD 215  USD215 In stock
50mg USD 300  USD300 In stock
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Quality Control & Documentation
Biological Activity

NSC 617145 is a selective werner syndrome helicase (WRN) helicase inhibitor,IC50 The value is 230 nM. NSC 617145 inhibit WRN ATPase and induce double-strand rupture (DSB) and chromosomal abnormalities. NSC 617145 is selective to WRN and superior to BLM, FANCJ, ChlR1, RecQ, and UvrD helicases.

Chemical Information
Molecular Weight 400.04
Formula C13H10Cl4N2O4
CAS Number 203115-63-3
Solubility (25°C) DMSO ≥ 10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] R Moles, et al. J Hematol Oncol. WRN-targeted therapy using inhibitors NSC 19630 and NSC 617145 induce apoptosis in HTLV-1-transformed adult T-cell leukemia cells

[2] Monika Aggarwal, et al. Cell Cycle. Targeting an Achilles' heel of cancer with a WRN helicase inhibitor

[3] Monika Aggarwal, et al. Cancer Res. Werner syndrome helicase has a critical role in DNA damage responses in the absence of a functional fanconi anemia pathway

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