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Cat. No.: HY-118269

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OSI-296

OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated.

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

CAS No.: 1175296-94-2
Formula: C₂₁H₁₉Cl₂FN₄O₃
Molecular Weight:465.30

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

OSI-296 Chemical Structure

CAS No.: 1175296-94-2

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Fluorescent Dye

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

Biological Activity
- Description
- Cellular Effect
Chemical Information
Purity & Documentation
References
Calculators
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Bioz

Biological Activity

Description

OSI-296 is a potent, oral and selective inhibitor of cMET and RON kinases. OSI-296 shows in vivo efficacy in MKN45 tumor xenografts models and well tolerated^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	0.2 μM Compound: 6, OSI-296	Inhibition of short-form RON (unknown origin) expressed in human HeLa cells assessed as phosphorylated RON levels after 4 hrs Inhibition of short-form RON (unknown origin) expressed in human HeLa cells assessed as phosphorylated RON levels after 4 hrs	[PMID: 23773865]
HT-29	IC₅₀	>10 μM Compound: 6, OSI-296	Inhibition of aurora-B in human HT-29 cells assessed as phosphorylation of histone H3 at Ser10 in presence of mouse plasma Inhibition of aurora-B in human HT-29 cells assessed as phosphorylation of histone H3 at Ser10 in presence of mouse plasma	[PMID: 23773865]
HT-29	IC₅₀	1 μM Compound: 6, OSI-296	Inhibition of aurora-B in human HT-29 cells assessed as phosphorylation of histone H3 at Ser10 Inhibition of aurora-B in human HT-29 cells assessed as phosphorylation of histone H3 at Ser10	[PMID: 23773865]
HUVEC	IC₅₀	6.1 μM Compound: 6, OSI-296	Inhibition of KDR autophosphorylation in HUVEC Inhibition of KDR autophosphorylation in HUVEC	[PMID: 23773865]
KARPAS-299	IC₅₀	0.5 μM Compound: 6, OSI-296	Inhibition of ALK autophosphorylation in human Karpas-299 cells Inhibition of ALK autophosphorylation in human Karpas-299 cells	[PMID: 23773865]
MKN-45	ED₅₀	50 mg/kg Compound: 6, OSI-296	Antitumor activity against human MKN45 cells xenografted in po dosed nu/nu CD1 mouse model assessed as tumor growth inhibition administered qd for 14 days Antitumor activity against human MKN45 cells xenografted in po dosed nu/nu CD1 mouse model assessed as tumor growth inhibition administered qd for 14 days	[PMID: 23773865]
MKN-45	IC₅₀	0.042 μM Compound: 6, OSI-296	Inhibition of cMET in human MKN45 cells assessed as phosphorylated MET levels after 4 hrs Inhibition of cMET in human MKN45 cells assessed as phosphorylated MET levels after 4 hrs	[PMID: 23773865]
MKN-45	IC₅₀	0.13 μM Compound: 6, OSI-296	Antiproliferative activity against human MKN45 cells after 3 days by CellTiter-Glo assay Antiproliferative activity against human MKN45 cells after 3 days by CellTiter-Glo assay	[PMID: 23773865]
MKN-45	IC₅₀	0.6 μM Compound: 6, OSI-296	Inhibition of cMET in human MKN45 cells assessed as phosphorylated MET levels after 4 hrs in presence of mouse plasma Inhibition of cMET in human MKN45 cells assessed as phosphorylated MET levels after 4 hrs in presence of mouse plasma	[PMID: 23773865]

Chemical Information

CAS No. 1175296-94-2
Molecular Weight 465.30
Formula C₂₁H₁₉Cl₂FN₄O₃
SMILES

O=C(N)N1CC=C(CC1)C2=COC3=C2C=NC(N)=C3O[C@H](C)C4=C(C=CC(F)=C4Cl)Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 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)

References

[1]. Steinig AG, et al. Novel 6-aminofuro[3,2-c]pyridines as potent, orally efficacious inhibitors of cMET and RON kinases. Bioorg Med Chem Lett. 2013;23(15):4381-4387. [Content Brief]

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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.

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100 mg

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