1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. SYN1143

SYN1143 

Cat. No.: HY-18307
Handling Instructions

SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated.

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

SYN1143 Chemical Structure

SYN1143 Chemical Structure

CAS No. : 913376-84-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 245 In-stock
Estimated Time of Arrival: December 31
5 mg USD 200 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
25 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1300 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively. SYN1143 has weak inhibitory activity on Lck, Tie2, Src, and BTK with IC50s ranging from 160 to 710 nM. SYN1143 can be used for the research of cancers that RON and c-Met are activated[1].

IC50 & Target[1]

c-Met

4 nM (IC50)

RON

9 nM (IC50)

In Vitro

SYN1143 (Compound I) (10-1000 nM; 1 h) inhibits c-Met-mediated signaling and functional activity in HT-29 and BxPC3 cells[1].
SYN1143 (10-1000 nM; 1 h) inhibits RON-mediated signaling and functional activity in NIH3T3 RON and BxPC3 cells[1].
SYN1143 (0.3-30 μM; 2 h or 3 d) inhibits c-Met signaling and cell proliferation in MC3T3-E1 and C3H10T1/2 cells[2].
SYN1143 (0.3-2 μM; 4-12 d) potentiates osteogenic differentiation of precursor cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: HT-29 and BxPC3 cells
Concentration: 10, 30, 100, 300, 1000 nM
Incubation Time: 1 hours
Result: Inhibited HGF-mediated c-Met phosphorylation and downstream signaling in a dose-dependent manner in both cell lines.
In Vivo

SYN1143 (10-100 mg/kg; p.o. for 22 d) inhibits the growth of c-Met-dependent and constitutively active RON-expressing tumors in mice[1].
SYN1143 (20-50 μg; transferred into calvarial defects) stimulates bone formation in critical-sized defects of mouse calvarial bone[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CD1 nu/nu mice (6-8 weeks) bearing NIH3T3 TPR-Met s.c. tumors[1]
Dosage: 10, 30, 100 mg/kg
Administration: Oral gavage either once or twice daily for 22 days
Result: Significantly inhibited tumor growth at doses of 30 or 100 mg/kg once daily or at 30 mg/kg twice daily.
Completely inhibited tumor growth at a dose of 100 mg/kg once daily.
Did not adversely affect body weight.
Molecular Weight

556.58

Formula

C₃₁H₂₉FN₄O₅

CAS No.

913376-84-8

SMILES

O=C(C1=C(C)N(CC(C)(O)C)N(C2=CC=CC=C2)C1=O)NC3=CC=C(OC4=CC=NC5=CC(OC)=CC=C45)C(F)=C3

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 : 100 mg/mL (179.67 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7967 mL 8.9834 mL 17.9669 mL
5 mM 0.3593 mL 1.7967 mL 3.5934 mL
10 mM 0.1797 mL 0.8983 mL 1.7967 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: 2.5 mg/mL (4.49 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.49 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.49 mM); Clear solution

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

SYN1143SYN 1143SYN-1143c-Met/HGFRdualc-MetRONcancertumorInhibitorinhibitorinhibit

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