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Art. -Nr.: HY-151461

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CHNQD-01255

CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy.

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CAS. Nr.: 2756173-91-6
Formel: C₂₃H₂₉NO₆
Molecular Weight:415.48

Speicherung:

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

Data Sheet (273 KB)

CHNQD-01255 Chemical Structure

CAS. Nr.: 2756173-91-6

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
Bel-7402	IC₅₀	0.07 μM Compound: 16; CHNQD-01255	Antiproliferative activity against human Bel-7402 cells by MTT assay Antiproliferative activity against human Bel-7402 cells by MTT assay	[PMID: 36089748]
HepG2	IC₅₀	0.1 μM Compound: 16; CHNQD-01255	Antiproliferative activity against human HepG2 cells by MTT assay Antiproliferative activity against human HepG2 cells by MTT assay	[PMID: 36089748]

In Vitro

CHNQD-01255 (0-1 μM approximately, 72 h) inhibits HepG2 and BEL-7402 cell proliferation^[1].

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

Cell Proliferation AssayCHNQD-01255 (0-1 μM approximately, 72 h) inhibits HepG2 and BEL-7402 cell proliferation^[1].

Cell Line:

HepG2, BEL-7402 cell
Concentration:

0-1 μM approximately
Incubation Time:

72 h
Result:

Inhibited cell proliferation with an IC₅₀ value of 0.1 μM (HepG2) and 0.07 μM (BEL-7402).

In Vivo

CHNQD-01255 (5- 45 mg/kg, p.o.) inhibits tumor growth in HepG2 tumor-bearing xenograft mice^[1].
CHNQD-01255 exhibits a high safety profile with MTD values exceeding 750 and 100 mg/kg for p.o. and i.p. administrations in mice^[1].

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

Animal Model:

HepG2 tumor-bearing xenograft mice^[1]
Dosage:

5, 15, and 45 mg/kg
Administration:

Oral adminstration (p.o.), every day for 21 consecutive days.
Result:

Resulted in dramatically delayed tumor progression, with a tumor growth inhibition rate (TGI %) value of 61.0% at 45 mg/kg.

Animal Model:

HepG2 tumor-bearing xenograft mice^[1]
Dosage:

1 and 9 mg/kg
Administration:

Intraperitoneal injection (i.p.), every day for 21 consecutive days.
Result:

Inhibited the tumor growth with the TGI values of 36.6 and 48.3%, respectively.

Animal Model:

Mice (Pharmacokinetic assay)^[1]
Dosage:

45 mg/kg p.o., 10 mg/kg i.v.
Administration:

Oral adminstration (p.o.) or intravenous injection (i.v.)
Result:

Pharmacokinetic profile of CHNQD-01255.

dose (mg/kg) T_1/2 (h) C_max (ng/mL) Cl (mL/h/kg) F (%)

45 (p.o.) 7.35 20.26 598245.37 2.26

10 (i.v.) 2060.78

Chemical Information

CAS. Nr. 2756173-91-6
Molecular Weight 415.48
Formel C₂₃H₂₉NO₆
SMILES

O[C@H]1[C@@]2([H])[C@@](/C=C/CCC[C@@H](OC(/C=C/1)=O)C)([H])C[C@@H](C2)OC(OCC3=CN=CC=C3)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 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)

Verweise

[1]. Yao-Yao Jiang, et al. Design and Characterization of a Natural Arf-GEFs Inhibitor Prodrug CHNQD-01255 with Potent Anti-Hepatocellular Carcinoma Efficacy In Vivo. J Med Chem. 2022 Sep 22;65(18):11970-11984. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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

100 mg

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