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Procarbazine HCl

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Chemical Structure| 366-70-1 同义名 : 盐酸丙卡巴肼 ;Procarbazine (hydrochloride);NSC-77213 HCl;NSC 77213;Natulan;Matulane®;Indicarb;Procarbazine Hydrochloride
CAS号 : 366-70-1
货号 : A775952
分子式 : C12H20ClN3O
纯度 : 98%
分子量 : 257.76
MDL号 : MFCD00072082
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(62.07 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(387.96 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Procarbazine Hydrochloride is an alkylating agent, with anticancer activity. Procarbazine is not cytotoxic to the LI 210 cells which lack cytochrome P-450 or monoamine oxidase activity. The azoxy isomers of procarbazine were metabolized in L1210 cells, presumably leading to the DNA or cytotoxic damage observed[3]. At 50 mg kg(-1), procarbazine induced micronuclei in hematopoietic cells, but it did not increase the lacZ mutant frequency (MF) in bone marrow[4]. Mice were orally exposed to PCH (Procarbazine Hydrochloride) (0, 6.25, 12.5, and 25 mg/kg/day) for 28 consecutive days. Blood samples collected 2 days after cessation of treatment exhibited significant dose-related induction of micronuclei in both immature and mature erythrocytes[5]. Procarbazine Hydrochloride (50 mg/kg, i.p.) causes micronuclei in hematopoietic cells, but does not increase the lacZ mutant frequency (MF) in bone marrow of mice, similar to that in liver, testis, spleen, kidney, and lung. Procarbazine Hydrochloride (50 mg/kg, i.p.) has positive effect on lung, bone marrow, and spleen for carcinogenesis[2]. Procarbazine (450 mg/kg) significantly decreases testicular and epididymal weight and drastically reduces haploid cells and spermatogenic arrest in hamster[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00431561 Glioblastoma ... 展开 >>Anaplastic Astrocytoma 收起 << Phase 2 Completed - Austria ... 展开 >> Universitätsklinik Innsbruck; Abteilung für Neurochirurgie Innsbruck, Austria, 6020 Landes-Nervenklinik Wagner-Jauregg Linz, Austria, 4020 Kaiser Franz Josef Spital, Abteilung für Neurologie Wien, Austria, 1100 Georgia Sarajishvili Institute of Clinical Neurology and Neurosurgery Tbilisi, Georgia, 0114 Germany Medizinische Klinik und Poliklinik mit Schwerpunkt Onkologie und Hämatologie, Charité Campus Mitte Berlin, Germany, 10117 Klinik und Poliklinik für Neurologie Cottbus, Germany, 03048 Universitätsklinikum Carl Gustav Carus an der Technischen Universität Dresden Dresden, Germany, 01307 Universitätsklinikum Gießen, Neurochirurgische Universitätsklinik Gießen, Germany, 35392 Universitätsklinikum Kiel, Klinik für Neurochirurgie Kiel, Germany, 24106 Universitätsklinikum Leipzig, Klinik und Poliklinik für Neurochirurgie Leipzig, Germany, 04103 Universitätsklinik Magdeburg, Klinik für Neurochirurgie Magdeburg, Germany, 39120 Universitätskliniken Mainz, Neurochirurgische Klinik und Poliklinik Mainz, Germany, 55131 Universitätsklinikum Münster, Klinik und Poliklinik für Neurochirurgie Münster, Germany, 48149 Klinikum und Poliklinik für Neurologie, Universität Regensburg Regensburg, Germany, 93053 Klinikum Saarbrücken, Neurochirurgie Saarbrücken, Germany, 66119 Neurologische Universitätsklinik Tübingen Tübingen, Germany, 72076 India Department of Neurosurgery, Amrita Institute of Medical Sciences & Research Centre Cochin, Kerala, India, 682026 Sree Chitra Tirunal Institute for Medical Sciences & Technology, Department of Neurosurgery Trivandrum, Kerala, India, 695011 Manipal Hospital; Manipal Institute for Neurological Disorders Bangalore, India, 560017 Department of Neurosurgery, National Institute of Mental Health and Neurosciences Bangalore, India, 560029 Department of Medical Oncology, Nizam's Institute of Medical Sciences Hyderabad, India, 500082 Department of Neurosurgery, LTMG Hospital & LTM Medical College Mumbai, India, 400022 Department of Neurosurgery, Neurosciences Center New Dehli, India, 110029 Department of Neurological Sciences, Christian Medical College & Hospital Vellore, India, 632004 Israel Soroka Medical Center, Neurosurgery Department Beer Sheva, Israel Rambam Medical Center, Neurosurgery Department Haifa, Israel, 31096 Rabin Medical Center, Neurosurgery Department Petach Tikva, Israel, 49100 Russian Federation Sverdlovsk Regional Oncological Clinic Ekaterinburg, Russian Federation, 620036 Republican Clinical Hospital of Ministry of Health of Tatarstan Republic Kazan, Russian Federation, 420064 Burdenko Neurosurgery Research Institute Moscow, Russian Federation, 125047 Omsk State Medical Academy; State Educational Institution of Higher Professional Education Omsk, Russian Federation, 644099 State Institution of Healthcare, Samara Regional Clinical Hospital in the name of M.I. Kalinin Samara, Russian Federation, 443095 Polenov Neurosurgery Research Institute St. Petersburg, Russian Federation, 191104 Military Medical Academy named after I.S.M. Kirov, Neurosurgery Department St. Petersburg, Russian Federation, 194175 Medical Center "XXI century" St. Petersburg, Russian Federation, 194354 Tcheliabinsk Regional Clinical Hospital; State Medical Institution for Prophylaxis and Treatment Tcheliabinsk, Russian Federation, 454076 收起 <<
NCT00592111 Pediatric Hod... 展开 >>gkin's Disease 收起 << Phase 2 Completed - United States, New York ... 展开 >> Memorial Sloan Kettering Cancer Center New York, New York, United States, 10065 收起 <<
NCT00264953 Hodgkin´s Lymphoma Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.88mL

0.78mL

0.39mL

19.40mL

3.88mL

1.94mL

38.80mL

7.76mL

3.88mL
参考文献

[1]Kraft SL, Baker NM, et al. Procarbazine and antidepressants: a retrospective review of the risk of serotonin toxicity. Psychooncology. 2014 Jan;23(1):108-13.

[2]Ogawa K, Hiraku Y, et al. Molecular mechanisms of DNA damage induced by procarbazine in the presence of Cu(II). Mutat Res. 2003 Aug 5;539(1-2):145-55.

[3]Erikson JM, Tweedie DJ, Ducore JM, Prough RA. Cytotoxicity and DNA damage caused by the azoxy metabolites of procarbazine in L1210 tumor cells. Cancer Res. 1989 Jan 1;49(1):127-33

[4]Suzuki T, Uno Y, Idehara K, Baba T, Maniwa J, Ohkouchi A, Wang X, Hayashi M, Sofuni T, Tsuruoka M, Miyajima H, Kondo K. Procarbazine genotoxicity in the MutaMouse; strong clastogenicity and organ-specific induction of lacZ mutations. Mutat Res. 1999 Aug 18;444(2):269-81

[5]Maurice C, Dertinger SD, Yauk CL, Marchetti F. Integrated In Vivo Genotoxicity Assessment of Procarbazine Hydrochloride Demonstrates Induction of Pig-a and LacZ Mutations, and Micronuclei, in MutaMouse Hematopoietic Cells. Environ Mol Mutagen. 2019 Jul;60(6):505-512

[6]Weissenberg R, Golan R, Shochat L, Lewin LM. Procarbazine effects on spermatogenesis in golden hamster: a flow cytometric evaluation. Arch Androl. 2002 Mar-Apr;48(2):91-100