CSF1R-IN-2

SKU: orb1218384

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).

Research Area

Signal Transduction

Key Properties

• CAS Number: 2271119-26-5
• MW: 409.42
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₀FN₇O₂
• SMILES: N#CC1=C2CN(CC)C(C=C3)=NC(N3N=C4N)=C4C(NC[C@H](C)OC2=CC=C1F)=O
• Target: Src
• Solubility: DMSO:25 mg/mL (61.06 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Elzovantinib (TPX-0022; p.o. , BID, 13 days) treatment results in an 85% tumor regression and no body weight loss is observed after 21 days treatment in mice. Elzovantinib (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 SCID/Beige mice. Elzovantinib inhibits MET activity in MKN-45 tumors following oral administration in mice. Animal model: Mice bearing LU2503 tumors patient derived xenograft (PDX) NSCLC model. Dosage: 15 mg/kg. Administration: PO, BID (twice daily) for 13 days. Result: Resulted in an 85% tumor regression and no body weight loss was observed after 21 days treatment. Animal model: SCID/Beige mice bearing Ba/F3 ETV6-CSF1R tumors with average tumor size of ~180 mm3. Dosage: 5 and 15 mg/kg. Administration: PO, BID (twice daily) for 10 days. Result: Demonstrated the ability to inhibit tumor growth at 44% and 67% at the dose of 5 mg/kg, BID and 15 mg/kg, BID, respectively.
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• In Vitro:
  Elzovantinib (TPX-0022) causes the suppression of MET autophosphorylation as well as the downstream STAT3, 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: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Src