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

OSI-930 

Cat. No.: HY-10204 Purity: 98.13%
Handling Instructions

OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.

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
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 132 In-stock
Estimated Time of Arrival: December 31
Solid
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  

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Customer Review

Based on 3 publication(s) in Google Scholar

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Description

OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity[1].

IC50 & Target[1]

KDR

9 nM (IC50)

Flt-1

8 nM (IC50)

Kit

80 nM (IC50)

PDGFRβ

6900 nM (IC50)

PDGFRα

3408 nM (IC50)

CSF-1R

15 nM (IC50)

c-Raf

41 nM (IC50)

Flt-3

1303 nM (IC50)

Lck

22 nM (IC50)

Abl

4738 nM (IC50)

In Vitro

OSI-930 inhibits cell proliferation in the HMC-1 cell line with IC50 of 14 nM but has no significant effect on the growth of COLO-205 cell line that does not express constitutively active mutant receptor tyrosine kinase[1]. OSI-930 induces apoptosis in HMC-1 cell line with an EC50 value of 34 nM[1]. OSI-930 inactivates purified, recombinant cytochrome P450 3A4 with a Ki of 24 μM in a time- and concentration-dependent manner[2]

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

In Vivo

OSI-930 (oral gavage; once a day; 38 days; 200 mg/kg) exhibits potent antitumor activity in a broad range of preclinical xenograft models[1].

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

Animal Model: Female nu/nu CD-1 mice bearing HMC-1, NCI-SNU-5, COLO-205 and U251 xenograft models[1]
Dosage: 200 mg/kg
Administration: Oral gavage; once a day; 38 days
Result: Showed a significant level of inhibition of Kit, KDR and CSF-1R.
Clinical Trial
Molecular Weight

443.44

Formula

C₂₂H₁₆F₃N₃O₂S

CAS No.
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)

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