An FMS inhibitor
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AZD 7507

Item No. 37485

Technical Information
Formal Name
4-[(2-fluoro-4-methylphenyl)amino]-6-[4-(2-hydroxyethyl)-1-piperazinyl]-7-methoxy-3-cinnolinecarboxamide
CAS Number
1041852-85-0
Molecular Formula
C23H27FN6O3
Formula Weight
Purity
≥98%
A solid
λmax
292, 365 nm
SMILES
O=C(C1=C(NC2=CC=C(C)C=C2F)C3=C(C=C(C(N4CCN(CC4)CCO)=C3)OC)N=N1)N
InChi Code
InChI=1S/C23H27FN6O3/c1-14-3-4-17(16(24)11-14)26-21-15-12-19(30-7-5-29(6-8-30)9-10-31)20(33-2)13-18(15)27-28-22(21)23(25)32/h3-4,11-13,31H,5-10H2,1-2H3,(H2,25,32)(H,26,27)
InChi Key
CPDGCAFPSYOTGO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    AZD 7507 is an inhibitor of CSF-1 receptor tyrosine kinase (FMS; IC50 = 3 nM).1 It is selective for FMS over c-KIT, NUAK1, FMS-related tyrosine kinase 4 (FLT4), p90 ribosomal S6 kinase (RSK1), and 77 other kinases at 1 µM. AZD 7505 (100 nM) induces apoptosis in isolated Fms+ mouse bone marrow cells but not Fms- mouse bone marrow cells. In vivo, AZD 7505 (100 mg/kg per day) reduces the levels of tumor-associated Fms+ macrophages, increases the number of tumor-associated CD8+ T cells, decreases tumor weight, and increases survival in a UN-KPC-960 murine model of pancreatic ductal adenocarcinoma (PDAC). It decreases α-smooth muscle actin (α-Sma) levels and increases E-cadherin levels on isolated UN-KPC-960 tumor tissue, as well as reduces the levels of Ifn-γ, Il-10, Il-17a, chemokine (C-X-C motif) ligand 2 (Cxcl2), chemokine (C-C motif) ligand 2 (Ccl2), Ccl7, and Ccl12 in protein lysates from the same tumors.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Candido, J.B., Morton, J.P., Bailey, P., et alCSF1R+ macrophages sustain pancreatic tumor growth through T cell suppression and maintenance of key gene programs that define the squamous subtype. Cell Rep. 23(5), 1448-1460 (2018).