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製品番号: 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 番号: 2097497-16-8
分子式: C₁₉H₁₅N₃O₂
分子量:317.34

保管条件:

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

Data Sheet (275 KB)

Anticancer agent 109 構造式

CAS 番号: 2097497-16-8

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

Axl

TAM Receptor アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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.

体内実験

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.

化学情報

CAS 番号 2097497-16-8
分子量 317.34
分子式 C₁₉H₁₅N₃O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (275 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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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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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MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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Anticancer agent 109

TAM Receptor アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Anticancer agent 109 関連分類

HY-149092 関連分類