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Cat. No.: HY-151404

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Antitumor agent-76

Antitumor agent-76 (Compound TP-P1) is an orally active, rapid-release and water-soluble Triptolide (HY-32735) proagent with antitumor activity.

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CAS No.: 2787593-12-6
Formule: C₂₈H₃₆ClNO₁₀
Masse moléculaire:582.04

Stockage:

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

Data Sheet (279 KB)

Antitumor agent-76 Chemical Structure

CAS No.: 2787593-12-6

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

Activité biologique

Description

Antitumor agent-76 (Compound TP-P1) is an orally active, rapid-release and water-soluble Triptolide (HY-32735) proagent with antitumor activity^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC₅₀	45.97 nM Compound: TP-P1	Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition measured after 48 hrs by CCK8 assay	[PMID: 36115206]
THP-1	IC₅₀	14.79 nM Compound: TP-P1	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth measured after 48 hrs by CCK8 assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth measured after 48 hrs by CCK8 assay	[PMID: 36115206]

In Vitro

Antitumor agent-76 (Compound TP-P1) shows good stability in aqueous solution, and the aqueous solubility (6.13 mg/mL in water) improved significantly compared to Triptolide^[1].
Antitumor agent-76 (50 μg/mL) can be rapidly and completely converted into Triptolide within 30 min in rat plasma and within 45 min in human plasma. The concentration of Antitumor agent-76 has no significant effect on conversion rate^[1].
Antitumor agent-76 (30-120 nM; 24 h) shows antiproliferative activities against acute myeloid leukemia (AML) cells without cytotoxicity towards normal cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

THP-1 and MV-4-11 cells
Concentration:

30, 60, or 120 nM
Incubation Time:

24 h
Result:

Showed antiproliferative activities with IC₅₀s of 14.79±0.42 nM and 45.97±0.13 nM against THP-1 and MV-4-11 cells, respectively.

In Vivo

Antitumor agent-76 (Compound TP-P1) (0-1.2 mg/kg; i.p.; daily for 28 days) inhibits tumor cell growth, proliferation and induces tumor cell apoptosis in mouse THP-1 and MV-4-11 xenografts models^[1].
Antitumor agent-76 (100, 300 μg/kg/day; i.g.; 11 days) dose-dependently inhibits tumor growth in mouse MV-4-11 xenograft models^[1].
Antitumor agent-76 is easily hydrolyzed in liver microsomes due to the high content of esterase in liver. The half-life is short (T_1/2=8.64 min) and the clearance rate is high^[1].
Pharmacokinetic study of Antitumor agent-76 (Compound TP-P1) and triptolide on Sprague Dawley rats^a^[1].

^aThe values presented are the mean values from three independent mice.
^bDosed po (oral administration) was administered via oral gavage.

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

Animal Model:

Male BALB/c Nude mice, THP-1 xenograft and MV-4-11 xenograft^[1]
Dosage:

0.1, 0.3, 0.6, 1.2 mg/kg for THP-1 xenograft, 25, 50, 100 μg/kg for MV-4-11 xenograft
Administration:

Intraperitoneal administration, daily for 28 days
Result:

Significantly and dose-dependently inhibited the tumor growth in THP-1 xenografts, with an excellent tumor growth inhibitory rate (TGI) of 93.87% at the dosage of 100 μg/kg. Inhibited cell proliferation and induced cell apoptosis in tumor tissues. Also showed excellent antitumor activity in MV-4-11 xenograft models (25 μg/kg with a TGI of 54.3%), and the tumors achieved complete regression on day 12 at the dosage of 100 μg/kg.

Animal Model:

Sprague Dawley rats^[1]
Dosage:

1.6 mg/kg
Administration:

Oral administration (Pharmacokinetic Analysis)
Result:

Exhibited an acceptable pharmacokinetic property.

Chemical Information

CAS No. 2787593-12-6
Masse moléculaire 582.04
Formule C₂₈H₃₆ClNO₁₀
SMILES

O=C1OCC2=C1CC[C@]3([C@]2(C[C@H]4[C@@]5([C@]36O[C@H]6[C@@H]7O[C@@]7([C@H]5OC(COC(CN8CCOCC8)=O)=O)C(C)C)O4)[H])C.Cl
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 (279 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]. Kang D, et al. Discovery of a novel water-soluble, rapid-release triptolide prodrug with improved drug-like properties and high efficacy in human acute myeloid leukemia. Eur J Med Chem. 2022 Sep 5;243:114694. [Content Brief]

Calculators

Calculateur de molarité

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

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Molecular Weight Molecular Weight

Calculateur de dilution

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

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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.

Keywords

100 mg

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

Compd	dosage^b (mg/kg)	AUC_(0-t) (h ng/ml)	T_max (h)	V_Z/F (L/kg)	CL_Z/F (L/h/kg)	C_max (μg/L)
Antitumor agent-76	1.6	60.46	0.50	37831.99	24563.25	23.53

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