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Cat. No.: HY-175700

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YCJ-02

YCJ-02 is a selective Topoisomerase I (Top I) inhibitor. YCJ-02 can inhibit cell proliferation and induce apoptosis and G2/M phase arrest. YCJ-02 can induce DNA damage and increaseγ-H2AX levels. YCJ-02 can promote Top I deqradation via a ubiquitin/26S proteasome pathway. YCJ-02 increases the expressions of pro-apoptotic proteins Bad, Bax, and cleaved caspase-3. YCJ-02 shows broad-spectrum antitumor activity. YCJ-02 can be used for the research of cancer, such as intrahepatic cholangiocarcinoma (ICC).

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CAS No.: 2260557-09-1
화학식: C₂₃H₁₉F₂N₃O₃
분자량:423.41

보관:

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

Data Sheet (277 KB)

YCJ-02 Chemical Structure

CAS No.: 2260557-09-1

사이즈

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재고

수량

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

Topoisomerase I

All Topoisomerase Isoforms :

In Vitro

YCJ-02 shows antitumor activities in HepG2, HuCCT1, BXPC-3, SW1990, HCT-116, SW480, A2780, HeLa, and MCF-7 cells with IC₅₀ values of 0.025, 0.079, 1.15, 0.20, 0.16, 0.12, 0.25, 0.79, and 1.08 μM, respectively^[1].
YCJ-02 inhibits proliferation in human HuCCT1, RBE, QBC-939, and mouse A/N, B/R ICC cells with IC₅₀ values of 0.079, 0.31, 0.35, 1.51, and 2.68 μM, respectively^[1].
YCJ-02 (0.25-1 μM, 72 h) inhibits colony formation in QBC-939 and HuCCT1 cells^[1].
YCJ-02 (0.25-1 μM, 24-48 h) induces G2/M phase arrest and apoptosis in QBC-939 and HuCCT1 cells^[1].
YCJ-02 (0.05-0.8 μM) dose-dependently inhibits the Top I enzyme activity and exhibits minimal inhibitory activity against Top II^[1].
YCJ-02 (0.125-1 μM, 48 h) reduces Top I levels in QBC-939 and HuCCT1 cells^[1].
YCJ-02 (0.125-1 μM, 48 h) induces DNA damage^[1].
YCJ-02 (0.125-1 μM) reduced the levels of AKT, p-AKT^ser473, mTORC1, p-mTORC1^ser2448, and Notch1 (NICD) in QBC-939 and A/N cells^[1].

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

Apoptosis Analysis^[1]

Cell Line:

QBC-939 and HuCCT1 cells
Concentration:

0.25, 0.5 and 1μM
Incubation Time:

24 and 48 h
Result:

Increased apoptotic rates.
Upregulated levels of p21, p53 and Bcl-2.

Western Blot Analysis^[1]

Cell Line:

QBC-939 and HuCCT1 cells
Concentration:

0.125, 0.25, 0.5 and 1μM
Incubation Time:

48 h
Result:

Reduced Top I levels.

Immunofluorescence^[1]

Cell Line:

QBC-939 cells
Concentration:

0.125, 0.25, 0.5 and 1μM
Incubation Time:

12 h
Result:

Reduced Top I levels.
Increased γ-H2AX levels.

In Vivo

YCJ-02 (10 mg/kg, i.p., 2 weeks for 10 times) inhibits tumor growth and prolongs survival in AKT/NICD-induced primary ICC mice models^[1].

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

Animal Model:

AKT/NICD-induced primary ICC mice models^[1]
Dosage:

10 mg/kg
Administration:

Intraperitoneally injection, 2 weeks for 10 times
Result:

Reduced tumor volume and prolonged survival.
Had no significant body weight loss.
Decreased tumor area.
Reduced the positive cell rates of CK19 and Ki-67.
Reduced Top I levels and increased the levels of p21, p53, cleaved caspase 3, and γ-H2AX.
Reduced p-AKT^ser473, mTORC1, p-mTORC1^ser2448, and Notch1 (NICD).

Chemical Information

CAS No. 2260557-09-1
분자량 423.41
화학식 C₂₃H₁₉F₂N₃O₃
SMILES

O=C1C2=CC(F)=C(C=C2C3=C(N1CCN4CCCC4)C5=CC6=C(OCO6)C=C5N=C3)F
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 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]. Yin-Peng Bai, et.al. A Difluorinated Derivative of ARC-111 Suppresses Intrahepatic Cholangiocarcinoma Growth via Targeting Topoisomerase I. ACS Pharmacol. Transl. Sci.

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
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YCJ-02

All Topoisomerase Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

YCJ-02 Related Classifications

HY-175700 Related Classifications