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ML216

Cat. No. M5047
ML216 Structure
Synonym:

CID-49852229

Size Price Availability Quantity
10mM*1mL USD 77  USD77 In stock
5mg USD 60  USD60 In stock
10mg USD 105  USD105 In stock
25mg USD 220  USD220 In stock
50mg USD 330  USD330 In stock
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Quality Control & Documentation
Biological Activity

ML216 shows cell-based activity, and can induce sister chromatid exchanges, enhance to the toxicity of aphidicolin and exert anti-proliferative activity in cells expressing BLM, but not in those lacking BLM.

Chemical Information
Molecular Weight 383.32
Formula C15H9F4N5OS
CAS Number 1430213-30-1
Solubility (25°C) 10 mM in DMSO
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] Yangyang Kong, et al. BLM helicase inhibition synergizes with PARP inhibition to improve the radiosensitivity of olaparib resistant non-small cell lung cancer cells by inhibiting homologous recombination repair

[2] Niranjan Suthram, et al. Elucidation of DNA Repair Function of PfBlm and Potentiation of Artemisinin Action by a Small-Molecule Inhibitor of RecQ Helicase

[3] Stefano Lazzarano, et al. Genetic mapping of species differences via in vitro crosses in mouse embryonic stem cells

[4] Andrew S. Rosenthal, et al. Discovery of ML216, a Small Molecule Inhibitor of Bloom (BLM) Helicase

[5] Giang Huong Nguyen, et al. A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells

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Keywords: ML216, CID-49852229 supplier, inhibitors, activators


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