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OTSSP167

Cat. No. M2902
OTSSP167 Structure
Synonym:

MELK inhibitor

Size Price Availability Quantity
5mg USD 180  USD180 In stock
10mg USD 290  USD290 In stock
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Quality Control & Documentation
Biological Activity

OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.

Chemical Information
Molecular Weight 487.42
Formula C25H28Cl2N4O2
CAS Number 1431697-89-0
Solubility (25°C) DMSO 10 mM
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] Bufu Tang, et al. Pharmacological inhibition of MELK restricts ferroptosis and the inflammatory response in colitis and colitis-propelled carcinogenesis

[2] Qinyang Xu, et al. MELK promotes Endometrial carcinoma progression via activating mTOR signaling pathway

[3] Josphine Muller, et al. Maternal embryonic leucine zipper kinase inhibitor OTSSP167 has preclinical activity in multiple myeloma bone disease

[4] Wenbin Ji, et al. OTSSP167 Abrogates Mitotic Checkpoint through Inhibiting Multiple Mitotic Kinases

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Keywords: OTSSP167, MELK inhibitor supplier, AMPK, inhibitors, activators


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