Glesatinib hydrochloride( MGCD-265 hydrochloride )

Catalog No. M10436 CAS No. 1123838-51-6

Glesatinib (MGCD-265) is a tyrosine kinase inhibitor that potently and selectively inhibits Met and Axl kinase.

Purity : >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Biological Information

Product Name

Glesatinib hydrochloride
Note

Research use only, not for human use.
Brief Description

Glesatinib (MGCD-265) is a tyrosine kinase inhibitor that potently and selectively inhibits Met and Axl kinase.
Description

Glesatinib (MGCD-265) is a tyrosine kinase inhibitor that potently and selectively inhibits Met and Axl kinase.Lung Cancer Phase 2 Clinical.
In Vitro

Glesatinib hydrochloride (MGCD265 hydrochloride; 0.01-5 μM; for 72 hours) results in a dose-dependent inhibition of cancer cell growth and shows the low IC50 value of 0.08 μM on NSCLC H1299 cells. Glesatinib hydrochloride (0.01, 0.1, 0.5, 1 μM) significantly increases by several-fold the percentage of apoptotic cells in NSCLC H1299 cells. Glesatinib hydrochloride has the cytotoxicity to P-gp overexpressing cancer cells KB-C2, SW620/Ad300, HEK293/ABCB1, and their parent cells KB-3-1, SW620, HEK293 cells with the IC50s fell between 5 and 10 μM. Glesatinib hydrochloride (1, 3 μM; 120 mins) increases the intracellular [3H]-Paclitaxel accumulation and inhibits [3H]-Paclitaxel efflux in cancer cell lines overexpressing P-gp. Glesatinib hydrochloride (0-40 μM) stimulates the ATPase activity of P-gp transporters in a dose-dependent manner.
In Vivo

Glesatinib hydrochloride (MGCD265 hydrochloride; 15 mg/kg/day; orally; 40 weeks) causes a significant decrease in tumor size. Animal Model:4?6-week old female balb/c athymic (nu/nu) mice with HCC827 NSCLC tumor xenografts Dosage:15 mg/kg Administration:Orally; daily; 40 weeks Result:Caused a significant decrease in tumor size.
Synonyms

MGCD-265 hydrochloride
Pathway

Tyrosine Kinase
Target

TAM Receptor
Recptor

TAM Receptor
Research Area

Cancer
Indication

Lung Cancer

Chemical Information

CAS Number

1123838-51-6
Formula Weight

655.1576
Molecular Formula

C31H27ClF2N5O3S2X
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 28 mg/mL
SMILES

COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=S)NC(=O)CC5=CC=C(C=C5)F)F.Cl
Chemical Name

Benzeneacetamide, 4-fluoro-N-[[[3-fluoro-4-[[2-[5-[[(2-methoxyethyl)amino]methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxy]phenyl]amino]thioxomethyl]-, hydrochloride (1:x)