1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. c-Fms
    c-Kit
    VEGFR
    Apoptosis
  3. OSI-930

OSI-930 

Cat. No.: HY-10204 Purity: 97.23%
Handling Instructions

OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl.

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

OSI-930 Chemical Structure

OSI-930 Chemical Structure

CAS No. : 728033-96-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 198 In-stock
Estimated Time of Arrival: December 31
50 mg USD 647 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

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Based on 3 publication(s) in Google Scholar

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Description

OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. IC50 value: 9 nM(VEGFR2); 15 nM(CSF1R); 80 nM (Kit activated) [1] Target: VEGFR2/Kit/CSF1R in vitro: OSI-930 inhibits the cell proliferation in the HMC-1 cell line with IC50 of 14 nM without significant effect on growth of the COLO-205 cell line that does not express a constitutively active mutant receptor tyrosine kinase. Moreover, OSI-930 also induces apoptosis in HMC-1 cell line with EC50 of 34 nM [1]. A recent study shows that OSI-930 inactivates purified, recombinant cytochrome P450 (P450) 3A4 with a Ki of 24 μM in a time- and concentration-dependent mode [2]. in vivo: OSI-930, administrated at the maximally efficacious dose of 200 mg/kg by oral gavage, exhibits potent antitumor activity in a broad range of preclinical xenograft models including HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models [1].

Clinical Trial
Molecular Weight

443.44

Formula

C₂₂H₁₆F₃N₃O₂S

CAS No.

728033-96-3

SMILES

O=C(C1=C(NCC2=CC=NC3=CC=CC=C23)C=CS1)NC4=CC=C(OC(F)(F)F)C=C4

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 : 50 mg/mL (112.75 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2551 mL 11.2755 mL 22.5510 mL
5 mM 0.4510 mL 2.2551 mL 4.5102 mL
10 mM 0.2255 mL 1.1275 mL 2.2551 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 (5.64 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.64 mM); Clear solution

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

OSI-930 | OSI930 | OSI 930 | c-Fms | c-Kit | VEGFR | Apoptosis | CSF-1 receptor | colony stimulating factor 1 receptor | CSF-1R | CSF1R | SCFR | CD117 | Vascular endothelial growth factor receptor | Inhibitor | inhibitor | inhibit

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Product name:
OSI-930
Cat. No.:
HY-10204
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