CSF1R-IN-2

SKU: orb1308994

Description

CSF1R-IN-2 is a potent, orally bioavailable small molecule inhibitor targeting SRC, MET, and c-FMS (CSF1R) kinases with sub-nanomolar IC50 values. It serves as a valuable research tool for investigating tumor proliferation, metastasis, and tumor-associated macrophage biology in both cellular and animal models of cancer and inflammatory diseases.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2271119-26-5
• MW: 409.42
• Purity: 99.71% (May vary between batches)
• Formula: C₂₀H₂₀FN₇O₂
• SMILES: CCN1Cc2c(O[C@@H](C)CNC(=O)c3c(N)nn4ccc1nc34)ccc(F)c2C#N
• Target: c-Met/HGFR,Src,c-Fms
• Solubility: DMSO:25 mg/mL (61.06 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:2 mg/mL (4.88 mM)

Bioactivity

• Target IC50:
  Src:0.12 nM |c-Fms:0.76 nM |MET:0.14 nM
• 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

c-Met/HGFR, cMet/HGFR, cMet, c-Met, colony stimulating factor 1 receptor, CSF1R IN 2, CSF1RIN2, CSF-1R-IN-2, CSF1R-IN-2, CSF-1R, CSF1R, CSF-1 receptor, cFms, c-FMS, c-Fms, inhibit, MET, HGFR, Inhibitor, Src, SRC

Compound Identifiers

PubChem CID

137455315