CAS 1185763-69-2|NVP-BVU972

Introduction：Basic information about CAS 1185763-69-2|NVP-BVU972, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. NVP-BVU972 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Synonyms

Common Name	NVP-BVU972
CAS Number	1185763-69-2	Molecular Weight	340.381
Density	1.4±0.1 g/cm3	Boiling Point	/
Molecular Formula	C₂₀H₁₆N₆	Melting Point	/
MSDS	/	Flash Point	/

Names

Name	6-[[6-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline
Synonym	More Synonyms

NVP-BVU972 BiologicalActivity

Description	NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.IC50 value: 14 nM [1]Target: MetNVP-BVU972 potently inhibits MET kinase but displays low inhibition against other kinases including the most closely related kinase RON with IC50 values of more than 1000 nM. NVP-BVU972 also suppresses constitutive MET phosphorylation in GTL-16 cells or HGF-stimulated MET phosphorylation in A549 cells with IC50 values of 7.3 nM and 22 nM, respectively. NVP-BVU972 potently prevents the growth of the MET gene amplified cell lines GTL-16, MKN-45 and EBC-1 with IC50 values of 66 nM, 82 nM and 32 nM, respectively. In line with their high frequency in the NVP-BVU972 screen, Y1230 and D1228 mutations give rise to dramatic shifts in the measured IC50 values for NVP-BVU972 in BaF3 cell line. Resistance triggered by V1155L is more limited to NVP-BVU972. A dose-dependent reduction in TPR-MET phosphorylation when applying NVP-BVU972 to BaF3 cells expressing wild-type TPR-MET. Both Y1230H and D1228A mutations abrogated the effect of NVP-BVU972 but not AMG 458. However, F1200I and L1195V interferes with the potency of NVP-BVU972 to prevent TPR-MET phosphorylation.
Related Catalog	Signaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFRResearch Areas >>Cancer
References	[1]. Tiedt, Ralph, et al. A Drug Resistance Screen Using a Selective MET Inhibitor Reveals a Spectrum of Mutations That Partially Overlap with Activating Mutations Found in Cancer Patients. Cancer Research (2011), 71(15), 5255-5264. [2]. Shin JS, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2013 Oct 31.

Description

NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.IC50 value: 14 nM [1]Target: MetNVP-BVU972 potently inhibits MET kinase but displays low inhibition against other kinases including the most closely related kinase RON with IC50 values of more than 1000 nM. NVP-BVU972 also suppresses constitutive MET phosphorylation in GTL-16 cells or HGF-stimulated MET phosphorylation in A549 cells with IC50 values of 7.3 nM and 22 nM, respectively. NVP-BVU972 potently prevents the growth of the MET gene amplified cell lines GTL-16, MKN-45 and EBC-1 with IC50 values of 66 nM, 82 nM and 32 nM, respectively. In line with their high frequency in the NVP-BVU972 screen, Y1230 and D1228 mutations give rise to dramatic shifts in the measured IC50 values for NVP-BVU972 in BaF3 cell line. Resistance triggered by V1155L is more limited to NVP-BVU972. A dose-dependent reduction in TPR-MET phosphorylation when applying NVP-BVU972 to BaF3 cells expressing wild-type TPR-MET. Both Y1230H and D1228A mutations abrogated the effect of NVP-BVU972 but not AMG 458. However, F1200I and L1195V interferes with the potency of NVP-BVU972 to prevent TPR-MET phosphorylation.

Related Catalog

Signaling Pathways >>Protein Tyrosine Kinase/RTK >>c-Met/HGFRResearch Areas >>Cancer

References

[1]. Tiedt, Ralph, et al. A Drug Resistance Screen Using a Selective MET Inhibitor Reveals a Spectrum of Mutations That Partially Overlap with Activating Mutations Found in Cancer Patients. Cancer Research (2011), 71(15), 5255-5264.

[2]. Shin JS, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2013 Oct 31.

Chemical & Physical Properties

Density	1.4±0.1 g/cm3
Molecular Formula	C₂₀H₁₆N₆
Molecular Weight	340.381
Exact Mass	340.143646
PSA	60.90000
LogP	2.12
Index of Refraction	1.745
InChIKey	RNCNPRCUHHDYPC-UHFFFAOYSA-N
SMILES	Cn1cc(-c2ccc3ncc(Cc4ccc5ncccc5c4)n3n2)cn1
Storage condition	-20℃

Safety Information

Hazard Codes	N

Synonyms

BVU972

cc-601

CS-0967

6-((6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl)methyl)quinoline

6-{[6-(1-Methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl}quinoline

3qti

Quinoline, 6-[[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]-

NVPBVU972

NVP-BVU972

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