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BLZ945

Chemical Structure : BLZ945

CAS No.: 953769-46-5

BLZ945 (Sotuletinib, BLZ-945)

Catalog No.: PC-43194Not For Human Use, Lab Use Only.

Sotuletinib (BLZ945) is a potent, selective, brain-penetrant CSF-1R inhibitor with biochemical IC50 of 1 nM, displays >3,200-fold selectivity over other kinases (c-Kit, PDGFR-β, Flt3, Abl, etc.).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Sotuletinib (BLZ945) is a potent, selective, brain-penetrant CSF-1R inhibitor with biochemical IC50 of 1 nM, displays >3,200-fold selectivity over other kinases (c-Kit, PDGFR-β, Flt3, Abl, etc.).
Sotuletinib (BLZ945) inhibits CSF-1-dependent proliferation in bone marrow-derived macrophages (BMDMs) with EC50 of 67 nM, and decreases CSF-1R phosphorylation.
Sotuletinib (BLZ945) blocks glioma progression and significantly improves survival, efficiently limits tumor progression combining with PD-1/PD-L1 blocking antibodies in neuroblastoma.

Physicochemical Properties

M.Wt 398.4787
Formula C20H22N4O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

2-Pyridinecarboxamide, 4-[[2-[[(1R,2R)-2-hydroxycyclohexyl]amino]-6-benzothiazolyl]oxy]-N-methyl-

References

1. Pyonteck SM, et al. Nat Med. 2013 Oct;19(10):1264-72.

2. Pass HI, et al. Oncotarget. 2016 Aug 30;7(35):56408-56421.

3. Mao Y, et al. Clin Cancer Res. 2016 Aug 1;22(15):3849-59.

4. Quail DF, et al. Science. 2016 May 20;352(6288):aad3018.

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