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

CSF1R-IN-2 

Cat. No.: HY-111787 Purity: 99.97%
Handling Instructions

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.

For research use only. We do not sell to patients.

CSF1R-IN-2 Chemical Structure

CSF1R-IN-2 Chemical Structure

CAS No. : 2271119-26-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 385 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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.
Molecular Weight

409.42

Formula

C₂₀H₂₀FN₇O₂

CAS No.

2271119-26-5

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (61.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4425 mL 12.2124 mL 24.4248 mL
5 mM 0.4885 mL 2.4425 mL 4.8850 mL
10 mM 0.2442 mL 1.2212 mL 2.4425 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.08 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.97%

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CSF1R-IN-2
Cat. No.:
HY-111787
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