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Cat. No.: HY-149092

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Anticancer agent 109

Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models.

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CAS No.: 2097497-16-8
Formule: C₁₉H₁₅N₃O₂
Masse moléculaire:317.34

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

Data Sheet (275 KB)

Anticancer agent 109 Chemical Structure

CAS No.: 2097497-16-8

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

Axl

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	4.2 μM Compound: 6-15	Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36921529]
CHO-K1	IC₅₀	54.5 μM Compound: 6-15	Cytotoxicity against CHO-K1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against CHO-K1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36921529]
DU-145	IC₅₀	1.1 μM Compound: 6-15	Cytotoxicity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36921529]
HEK293	IC₅₀	26.2 μM Compound: 6-15	Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36921529]
HT-29	IC₅₀	4.6 μM Compound: 6-15	Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36921529]
MCF7	IC₅₀	2 μM Compound: 6-15	Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36921529]
MDA-MB-231	IC₅₀	2.8 μM Compound: 6-15	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36921529]
PANC-1	IC₅₀	4 μM Compound: 6-15	Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human PANC-1 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36921529]
U-937	IC₅₀	6.7 μM Compound: 6-15	Cytotoxicity against human U-937 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Cytotoxicity against human U-937 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 36921529]

In Vitro

Anticancer agent 109 (10 μM,48 h) inhibits of Gas6 and Axl in A549, inhibits of Gas6-Axl axis related proteins, increases the sub-G1 fraction and promotes of late stage apoptosis without altering DNA synthesis in PANC-1^[1].

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

Cell Viability Assay^[1]

Cell Line:

MCF-7; PANC-1; MDA-MB-231 ; HT-29 ; DU145 ; U937 ; A549 ; PANC-1
Concentration:

30 μM
Incubation Time:

48 h
Result:

Inhibited the growth of cancer cells, and was up to 20-fold safer against normal cells and up to 5.4-fold more active than Sunitinib against the cancer cells.
Inhibited growth with IC₅₀s of 2.0 μM (MCF-7); 2.8 μM (MDA-MB-231); 4.6 μM (HT-29); 1.1 μM (DU145); 6.7 μM (U937); 4.2 μM (A549); 4.0 μM (PANC-1).

Apoptosis Analysis^[1]

Cell Line:

PANC-1
Concentration:

1 μM , 5 μM , 10 μM
Incubation Time:

48 h
Result:

Increased the sub-G1 fraction and induced late apoptosis.

Western Blot Analysis^[1]

Cell Line:

A549; PANC-1
Concentration:

10 μM
Incubation Time:

48 h
Result:

Inhibited Gas6 and Axl in A549 and PANC-1 cell, increased the expression ratio of Bax/Bcl-2 and inhibited p-PI3K and p-AKT in PANC-1 cell.

RT-PCR^[1]

Cell Line:

PANC-1
Concentration:

3 μM ;5 μM 10 μM
Incubation Time:

48 h
Result:

Inhibited Gas6 and Axl.

In Vivo

Anticancer agent 109 (3 mg/kg, intraperitoneal injection, A549 tumor model for 31 days, PANC-1 tumor model for 85 days, six times a week) reduced tumor size and weight significantly in xenograft models of nude mice^[1].

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

Animal Model:

A549 or PANC-1 xenografted in BALB/c-nu mice^[1].
Dosage:

1 mg/kg; 3 mg/kg
Administration:

Intraperitoneal injection (i.p.) 6 times a week
Result:

Promoted tumor regression to around a quarter with 1 mg/kg, smaller but not eliminated with 3 mg/kg in A549 models.
Promoted tumor regression to around a quarter with 3 mg/kg in PANC-1 models.

Chemical Information

CAS No. 2097497-16-8
Masse moléculaire 317.34
Formule C₁₉H₁₅N₃O₂
SMILES

O=C(/C(C1=C2C)=C\C3=NC4=C(C=CC=C4)C=C3)NC1=NC(C)=C2O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 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)
Instruction de manipulation (2659 KB)

Références

[1]. Bae D, et al. Antitumor effect of 3-(quinolin-2-ylmethylene)-4,6-dimethyl-5-hydroxy-7-azaoxindole down-regulating the Gas6-Axl axis. Eur J Med Chem. 2023 May 5;251:115274. [Content Brief]

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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Anticancer agent 109

Voir tous les produits spécifiques à Isoform TAM Receptor

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

Anticancer agent 109 Related Classifications

HY-149092 Related Classifications