CGP-15720 hydrochloride
CGP-15720 hydrochloride is an orally active imidazolinylurea compound with anticancer activity, which exhibits inhibitory effects on human bronchial carcinoma in nude mice and respiratory tract tumors induced by diethylnitrosamine in Syrian hamsters. CGP-15720 hydrochloride acts via a non-cytotoxic mode of action, reduces tumor area and tumor incidence, and prolongs the survival time of tumor-bearing animals. Its combination with Bleomycin (HY-108345) or CCNU (HY-13669) produces additive antitumor effects. CGP-15720 hydrochloride can be used in cancer-related research such as bronchogenic carcinoma and laryngeal carcinoma.
For research use only. We do not sell to patients.
- CAS No.: 76692-12-1
- Formula: C18H20ClN5O3
- Molecular Weight:389.84
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vivo
CGP 15720 (100 mg/kg; p.o.; 5 times per week; 20 doses total) hydrochloride inhibits the growth of subcutaneously transplanted human bronchial epidermoid carcinoma 'Hotz'/1908 in nu/nu Balb/c mice, with an inhibition rate of 69.9%, and prolongs the mean survival time[1].
CGP 15720 (10-100 mg/kg via p.o., 5 times per week for a total of 15 doses; or at 30 mg/kg via i.p., 5 times per week for a total of 15 doses) hydrochloride inhibits tumor growth in nu/nu Balb/c mice subcutaneously implanted with human undifferentiated bronchial carcinoma MBA/9812, with a maximum inhibition rate of 98.2%[1].
CGP 15720 (10-100 mg/kg; p.o./i.p.; once daily; for 4 consecutive days; 10-100 mg/kg) hydrochloride inhibits the growth of Ehrlich carcinoma, Yoshida ascites hepatoma AH66 and CrSa 180 sarcoma, with a maximum inhibition rate of 99.3%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BIO 8720 (inbred, female, 50-day-old)
Lak:LVG (Syr) (outbred, female, 50-day-old)[1] -
Dosage:0.3, 1, 3, 10, 30, 100, 300, 1000 mg/kg (oral)
0.3, 1, 3, 10, 30, 100 mg/kg (intraperitoneal)
30 mg/kg (survival) -
Administration:p.o.; 5 times weekly; 4 weeks
i.p.; 5 times weekly; 4 weeks
p.o.; daily for 4 weeks then 5 times weekly until death -
Result:Achieved dose‑dependent reductions in tumor area (54‑83 %) and tumor number (42‑60 %) following oral CGP‑15720 A dosing, and produced 49‑78 % tumor‑area reductions alongside 27‑50 % tumor‑number reductions via intraperitoneal administration.
Reached a treated‑to‑control mean tumor‑area ratio of 2.3 mm2 / 6.7 mm2 at 30 mg/kg oral dosage.
Decreased adenocarcinoma relative frequency from 34 % to 6 % and diminished mean adenocarcinoma area from 0.44 mm2 to 0.02 mm2 under 30 mg/kg oral dosing.
Prolonged mean animal survival to 12.3 weeks, compared with 7.0 weeks in the control group at 30 mg/kg oral dosage.
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Animal Model:nu/nu Balb/c (female)[1]
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Dosage:10, 30, 100 mg/kg (oral)
30 mg/kg (intraperitoneal) -
Administration:p.o.; 5 times weekly; 15 doses
i.p.; 5 times weekly; 15 doses -
Result:Achieved dose‑dependent mean tumor‑weight reductions for human MBA 9812 xenograft: oral dosing produced 72.8‑98.2 % weight reduction; intraperitoneal sterile neutral solution generated 73.9‑87.4 % reduction, while intraperitoneal CMC/propylene glycol solution yielded 71.9‑74.4 % reduction.
Obtained 58.8‑68.7 % tumor‑weight reduction by oral sterile neutral solution, and 58.1‑69.5 % reduction by oral CMC/propylene glycol solution across 10‑100 mg/kg dosage range.
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Animal Model:nu/nu Balb/c (female)[1]
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Dosage:10, 30, 100 mg/kg
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Administration:p.o./i.p.; daily; 4 days
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Result:Reduced Ehrlich ascites carcinoma volume by 64.2% at 100 mg/kg p.o., 40.3% at 30 mg/kg p.o., 25.0% at 10 mg/kg p.o., 98.4% at 100 mg/kg i.p., 98.8% at 30 mg/kg i.p., and 27.1% at 10 mg/kg i.p.
Reduced Yoshida ascites hepatoma AH66 volume by 93.4% at 100 mg/kg p.o., 38.8% at 30 mg/kg p.o., 18.0% at 10 mg/kg p.o., 99.3% at 100 mg/kg i.p., 95.2% at 30 mg/kg i.p., and 13.1% at 10 mg/kg i.p.
Reduced CrSa 180 ascites sarcoma volume by 36.7% at 100 mg/kg p.o., 24.6% at 30 mg/kg p.o., 32.8% at 10 mg/kg p.o., 65.5% at 100 mg/kg i.p., 39.0% at 30 mg/kg i.p., and 39.6% at 10 mg/kg i.p.
Chemical Information
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CAS No. 76692-12-1
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Molecular Weight 389.84
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Formula C18H20ClN5O3
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SMILES
O=C(O)C1=CC=C(NC(NCCN2CCN=C2C3=CC=NC=C3)=O)C=C1.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CGP-15720 hydrochloride Related Classifications
HY-129843 Related Classifications
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Keywords
- CGP-15720
- 76692-12-1
- CGP15720
- CGP 15720
- Drug Derivative
- epidermoid carcinoma
- bronchogenic carcinoma
- respiratory tract adenocarcinomatous tumors
- human bronchogenic carcinomas
- transplantable rodent ascites tumors
- respiratory system tumors
- papillary carcinoma
- Syrian hamsters
- larynx carcinoma
- nu/nu Balb/c mice
- Inhibitor
- inhibitor
- inhibit