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CSF1R-IN-2 is an oral-active SRC, MET and c-FMS inhibitor (IC50s: 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $38 | In Stock | |
5 mg | $93 | In Stock | |
10 mg | $133 | In Stock | |
25 mg | $248 | In Stock | |
50 mg | $371 | In Stock | |
100 mg | $527 | In Stock | |
1 mL x 10 mM (in DMSO) | $101 | In Stock |
Description | CSF1R-IN-2 is an oral-active SRC, MET and c-FMS inhibitor (IC50s: 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively). |
Targets&IC50 | MET:0.14 nM , Src:0.12 nM , c-Fms:0.76 nM |
In vitro | The suppression of MET autophosphorylation as well as the downstream STAT3 caused by CSF1R-IN-2, ERK and AKT phosphorylation at IC50 values of around 1-3 nM in SNU-5 and MKN-45 cell lines. |
In vivo | In mice, CSF1R-IN-2 (p.o., BID, 13 days) treatment results in an 85% tumor regression, and no bodyweight loss is observed after 21 days of treatment. In SCID/Beige mice. CSF1R-IN-2 (p.o., BID, 10 days) demonstrates the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID, and 15 mg/kg, BID, respectively. In mice, CSF1R-IN-2 inhibits MET activity in MKN-45 tumors following oral administration. |
Molecular Weight | 409.42 |
Formula | C20H20FN7O2 |
Cas No. | 2271119-26-5 |
Smiles | CCN1Cc2c(O[C@@H](C)CNC(=O)c3c(N)nn4ccc1nc34)ccc(F)c2C#N |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 25 mg/mL (61.06 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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