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Merestinib

Cat. No. M3767
Merestinib Structure
Synonym:

LY2801653

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
2mg USD 60  USD60 In stock
5mg USD 90  USD90 In stock
10mg USD 155  USD155 In stock
25mg USD 300  USD300 In stock
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Quality Control & Documentation
Biological Activity

Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM).

Chemical Information
Molecular Weight 552.53
Formula C30H22F2N6O3
CAS Number 1206799-15-6
Solubility (25°C) DMSO 30 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] Kawada I, et al. Cancer Res. Dramatic antitumor effects of the dual MET/RON small-molecule inhibitor LY2801653 in non-small cell lung cancer.

[2] Wu W, et al. Clin Cancer Res. Inhibition of tumor growth and metastasis in non-small cell lung cancer by LY2801653, an inhibitor of several oncokinases, including MET.

[3] Yan SB, et al. Invest New Drugs. LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models.

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Keywords: Merestinib, LY2801653 supplier, c-Met, inhibitors, activators


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