Art. -Nr.: HY-10204

OSI-930

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

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.

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Reinheit: 98.33%
CAS. Nr.: 728033-96-3
Formel: C₂₂H₁₆F₃N₃O₂S
Molecular Weight:443.44

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

OSI-930 Chemical Structure

CAS. Nr.: 728033-96-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

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 K_i of 24 μM in a time- and concentration-dependent manner^[2]

MedChemExpress (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].

MedChemExpress (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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 728033-96-3
Appearance Solid
Molecular Weight 443.44
Formel C₂₂H₁₆F₃N₃O₂S
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Commun Biol

ISX-9 potentiates CaMKIIδ-mediated BMAL1 activation to enhance circadian amplitude. [Abstract]

2022 Jul 28;5(1):750. PMID: 35902736
Drug Metab Dispos

Physiologically based pharmacokinetic modeling of aldehyde oxidase drug-drug interactions mediated by erlotinib. [Abstract]

2025 Jun 23;53(8):100113. PMID: 40683226

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (112.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Garton AJ, et al. OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res. 2006, 66(2):1015-1024. [Content Brief]

[2]. Lin HL, et al. Inactivation of cytochrome P450 (P450) 3A4 but not P450 3A5 by OSI-930, a thiophene-containing anticancer drug. Drug Metab Dispos. 2011, 39(2), 345-350. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2551 mL	11.2755 mL	22.5510 mL	56.3774 mL
	5 mM	0.4510 mL	2.2551 mL	4.5102 mL	11.2755 mL
	10 mM	0.2255 mL	1.1275 mL	2.2551 mL	5.6377 mL
	15 mM	0.1503 mL	0.7517 mL	1.5034 mL	3.7585 mL
	20 mM	0.1128 mL	0.5638 mL	1.1275 mL	2.8189 mL
	25 mM	0.0902 mL	0.4510 mL	0.9020 mL	2.2551 mL
	30 mM	0.0752 mL	0.3758 mL	0.7517 mL	1.8792 mL
	40 mM	0.0564 mL	0.2819 mL	0.5638 mL	1.4094 mL
	50 mM	0.0451 mL	0.2255 mL	0.4510 mL	1.1275 mL
	60 mM	0.0376 mL	0.1879 mL	0.3758 mL	0.9396 mL
	80 mM	0.0282 mL	0.1409 mL	0.2819 mL	0.7047 mL
	100 mM	0.0226 mL	0.1128 mL	0.2255 mL	0.5638 mL

Keywords

OSI-930

4 Cited Publications

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OSI-930

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Clinical Compound Library Plus

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Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) OSI-930

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

OSI-930 Related Classifications

HY-10204 Related Classifications