1. Protein Tyrosine Kinase/RTK
  2. Src
    c-Met/HGFR
    c-Fms
  3. CSF1R-IN-2

CSF1R-IN-2 

目录号: HY-111787
产品使用指南

CSF1R-IN-2 (compound 5) 是 SRCMETc-FMS 的口服有效抑制剂, 其对SRCMETc-FMSIC50 值分别为 0.12 nM,0.14 nM 和 0.76 nM。

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CSF1R-IN-2 Chemical Structure

CSF1R-IN-2 Chemical Structure

CAS No. : 2271119-26-5

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Description

CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively[1].

IC50 & Target

IC50: 0.12 nM (SRC), 0.14 nM (MET), 0.76 nM (c-FMS)[1].

In Vitro

CSF1R-IN-2 (compound 5) 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[1].

In Vivo

CSF1R-IN-2 (compound 5: 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[1].
CSF1R-IN-2 (compound 5: 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[1].
CSF1R-IN-2 (compound 5) inhibits MET activity in MKN-45 tumors following oral administration in mice[1].

Animal Model: Mice bearing LU2503 tumors patient derived xenograft (PDX) NSCLC model[1].
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[1].
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.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Molecular Weight

409.42

Formula

C₂₀H₂₀FN₇O₂

CAS No.

2271119-26-5

SMILES

N#CC1=C2CN(CC)C(C=C3)=NC(N3N=C4N)=C4C(NC[C@H](C)OC2=CC=C1F)=O

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Room temperature in continental US; may vary elsewhere

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产品名称:
CSF1R-IN-2
目录号:
HY-111787
需求量:

CSF1R-IN-2

Cat. No.: HY-111787