Belotecan hydrochloride - CAS 213819-48-8
Catalog number: B0084-087456
Category: Inhibitor
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Molecular Formula:
C25H28ClN3O4
Molecular Weight:
469.96
COA:
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Targets:
Topoisomerase
Description:
Belotecan hydrochloride, also called as CKD-602 hydrochloride, a Topoisomerase I inhibitor, is the hydrochloride salt of the semi-synthetic and water-soluble camptothecin analogue belotecan with potential antitumor activity.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-087456 20 mg $199 In stock
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Brife Description:
A Topoisomerase I inhibitor
Related CAS:
256411-32-2 (free base)
Synonyms:
7-(2-(N-isopropylamino)ethyl)camptothecin; belotecan; belotecan hydrochloride; CKD 602; CKD-602; CKD602
Solubility:
DMSO: ≥50 mg/mL
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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InChIKey:
SJKBXKKZBKCHET-UQIIZPHYSA-N
InChI:
1S/C25H27N3O4.ClH/c1-4-25(31)19-11-21-22-17(12-28(21)23(29)18(19)13-32-24(25)30)15(9-10-26-14(2)3)16-7-5-6-8-20(16)27-22;/h5-8,11,14,26,31H,4,9-10,12-13H2,1-3H3;1H/t25-;/m0./s1
Canonical SMILES:
CCC1(C2=C(COC1=O)C(=O)N3CC4=C(C5=CC=CC=C5N=C4C3=C2)CCNC(C)C)O.Cl
1.Preformulation studies of a novel camptothecin anticancer agent, CKD-602: physicochemical characterization and hydrolytic equilibrium kinetics.
Kim JH;Lee SK;Lim JL;Shin HJ;Hong CI Int J Pharm. 2002 Jun 4;239(1-2):207-11.
(20S)-7-(2-isopropylamino)ethylcamptothecin.HCl (CKD-602), a new camptothecin (CPT) anticancer agent, is a pale yellowish crystalline compound. DSC thermogram exhibited a melt endotherm near 270 degrees C, and CKD-602 was found to be slightly hygroscopic. The solubility of CKD-602 in deionized water was 8.22 mg/ml, and two pK(a) values were measured to be 2.32 and 9.15, respectively. A pH-dependent partition coefficient behavior in octanol-buffer was observed. CKD-602 in solid state was stable over the range of temperature and humidity, but decomposed slightly by light. The hydrolysis of CKD-602 occurred reversibly and rapidly in aqueous buffer solutions. The conversion rate constants (k(f): from the lactone to the carboxylate and k(r): from the carboxylate to the lactone) and the final equilibrium ratio (K(eq)) between two species were dependent on the pH of aqueous solutions.
2.Phase II study of belotecan, a camptothecin analogue, in combination with carboplatin for the treatment of recurrent ovarian cancer.
Choi CH;Lee YY;Song TJ;Park HS;Kim MK;Kim TJ;Lee JW;Lee JH;Bae DS;Kim BG Cancer. 2011 May 15;117(10):2104-11. doi: 10.1002/cncr.25710. Epub 2010 Nov 29.
BACKGROUND: ;Belotecan (CKD602; Camtobell, Chong Keun Dang Corp., Seoul, Korea) is a recently developed camptothecin derivative with antitumor properties. This phase II study was designed to evaluate the toxicity and efficacy of belotecan combined with carboplatin in patients with recurrent epithelial ovarian cancer (EOC).;METHODS: ;Thirty-eight patients with recurrent EOC were treated with belotecan 0.3 mg/m(2) /day (days 1-5) and carboplatin AUC 5 (day 5) every 3 weeks for 6 cycles. The primary objective was to determine the response rate as defined by Response Evaluation Criteria in Solid Tumors and CA-125 response. Other end points included toxicities and progression-free survival (PFS).;RESULTS: ;All 38 patients were assessed for toxicity, and 35 patients were assessed for response. The overall response rate was 57.1%; there were 7 complete responses (20.0%), 13 partial responses (37.1%), 6 patients with stable disease (17.1%), and 9 patients with progressive disease (25.7%). Grades 3 and 4 hematologic toxicities included neutropenia (28.8%), thrombocytopenia (19.8%), and anemia (14.4%), and there were 2 episodes of febrile neutropenia. Median PFS was 7 months, with a median follow-up of 12 months.
3.4-Week repeated intravenous dose toxicity study of a new camptothecin anticancer agent CKD-602 in dogs.
Kim JC;Shin DH;Park SH;Park SC;Kim YB;Kim HC;Cha SW;Cho KH;Kang BH;Chung MK Food Chem Toxicol. 2005 May;43(5):699-706.
CKD-602 is a new camptothecin derivative antitumor agent with a formula (7-[2-(N-isopropylamino)ethyl]-(20S)-camptothecin) developed by Chong Kun Dang Pharmaceutical Company in Korea. In the present study, the subacute toxicity of CKD-602 was investigated after 4-week repeated intravenous administration of the test chemical in beagle dogs. The test chemical was administered intravenously at dose levels of 0, 0.001, 0.005, or 0.01 mg/kg/day for 4 weeks to male and female dogs (n = 3 for male and female dogs for each dose). During the test period, clinical signs, mortality, body weights, food and water consumption, ophthalmoscopy, urinalysis, hematology, serum biochemistry, gross findings, organ weights and histopathology were examined. In the high dose group, an increase in the incidence of abnormal clinical signs and a decrease in food and water intake and body weight gain were observed in both sexes. Hematological investigations revealed decreased white blood cells (WBC) in both sexes and reduced red blood cells (RBC), hemoglobin and hematocrit in females. Histopathological examinations revealed an increase in the incidence of atrophy of the sternal and femoral marrow and spleen in both sexes and atrophy of the thymus and mesenteric lymph node in males.
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CAS 213819-48-8 Belotecan hydrochloride

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