|(2S)-2-(4-(((2-氨基-5-甲酰基-4-氧代-1,4,5,6,7,8-六氢蝶啶-6-基)甲基)氨基)苯甲酰胺基)戊二酸钙五水合物|CsnPharm

CAS No.: 6035-45-6

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 Catalog No. CSN11049

Synonyms: Leucovorin calcium salt pentahydrate;Folinic Acid;Leucovorin Calcium

Folinic acid is a reduced folic acid, which is used in combination with other chemotherapy drugs.

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实验方案

技术信息

生物活性

描述The biologically active form of folic acid is tetrahydrofolate which is essential for DNA synthesis. Tetrahydrofolate is oxidised to dihydrofolate during DNA synthesis and is regenerated to its active form by the enzyme dihydrofolate reductase. Inhibition of this enzyme prevents DNA synthesis and causes failure of cell renewal. This leads to breaks in epithelial surfaces resulting in oropharyngeal and intestinal ulceration. Methotrexate (MTX) is the most powerful antagonist to inhibit dihydrofolate reductase. Folinic acid is an analogue of tetrahydrofolate and so bypasses the dihydrofolate reductase block. It thus supplies the tetrahydrofolate compounds needed for DNA synthesis ^[3]. Treatment with folinic acid calcium pentahydrate (CF) could cause improved development in the heart and vessels in MTX-treated embryos, which proved that MTX induced the malformations by inhibiting dihydrofolate reductase (DHFR). The transcript levels of genes such as hand2, mef2a, mef2c, and flk-1 were reduced in MTX-treated embryos. Compared with the MTX-treated group, the transcript levels of hand2, mef2a, mef2c, and flk-1 were increased in the MTX + CF group ^[4]. Folinic Acid Calcium Pentahydrate may also be useful in the treatment of acute methotrexate overdose ^[3].
动物研究
剂量
Mice: 7 mg/kg^[3] (i.p.)

给药途径
i.p.
临床研究

动物研究
剂量	Mice: 7 mg/kg^[3] (i.p.)
给药途径	i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00720109	Adult B Acute Lymphoblastic Le... more >>ukemia With t(9;22)(q34;q11.2); BCR-ABL1 Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 Untreated Adult Acute Lymphoblastic Leukemia Untreated Childhood Acute Lymphoblastic Leukemia Collapse <<	Phase 2 Phase 3	Completed	-	-
NCT01256398	Acute Lymphoblastic Leukemia ... more >> Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 Untreated Adult Acute Lymphoblastic Leukemia Collapse <<	Phase 2	Active, not recruiting	-	-
NCT00720109	-	-	Completed	-	-

更多
参考文献

[1] Correale P, Cusi MG, et al. Dendritic cell-mediated cross-presentation of antigens derived from colon carcinoma cells exposed to a highly cytotoxic multidrug regimen with gemcitabine, oxaliplatin, 5-fluorouracil, and leucovorin, elicits a powerful human antigen-specific CTL response with antitumor activity in vitro. J Immunol. 2005 Jul 15;175(2):820-8.
[2] Van der Wilt CL, Pinedo HM, et al. Elevation of thymidylate synthase following 5-fluorouracil treatment is prevented by the addition of leucovorin in murine colon tumors. Cancer Res. 1992 Sep 15;52(18):4922-8.
[3] Calcium leucovorin - folinic acid rescue. Drug Ther Bull. 1978 Feb 3;16(3):11-2.
[4] Sun S, Gui Y, Wang Y, Qian L, Liu X, Jiang Q, Song H. Effects of methotrexate on the developments of heart and vessel in zebrafish. Acta Biochim Biophys Sin (Shanghai). 2009 Jan;41(1):86-96. doi: 10.1093/abbs/gmn010.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6623 mL
- 8.3115 mL
- 16.6230 mL
- 5 mM
- 0.3325 mL
- 1.6623 mL
- 3.3246 mL
- 10 mM
- 0.1662 mL
- 0.8311 mL
- 1.6623 mL

技术信息

CAS号

6035-45-6

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H31CaN7O12

运输

蓝冰

分子量

601.58

别名

Leucovorin calcium salt pentahydrate;Folinic Acid;Leucovorin Calcium;Leucovorin calcium hydrate;五水亚叶酸钙

溶解度

DMSO	insoluble
Water	160.0 mg/mL (266.0 mM) warming

动物实验配方

0.5% CMC-Na

80 mg/mL

clear

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00720109	Adult B Acute Lymphoblastic Le... more >>ukemia With t(9;22)(q34;q11.2); BCR-ABL1 Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34;q11.2); BCR-ABL1 Untreated Adult Acute Lymphoblastic Leukemia Untreated Childhood Acute Lymphoblastic Leukemia Collapse <<	Phase 2 Phase 3	Completed	-	-
NCT01256398	Acute Lymphoblastic Leukemia ... more >> Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 Untreated Adult Acute Lymphoblastic Leukemia Collapse <<	Phase 2	Active, not recruiting	-	-
NCT00720109	-	-	Completed	-	-
NCT00792948	-	-	Active, not recruiting	-	-
NCT02101853	B Acute Lymphoblastic Leukemia	Phase 3	Recruiting	-	-
NCT00792948	Acute Lymphoblastic Leukemia ... more >> Adult Acute Lymphoblastic Leukemia in Remission Adult B Acute Lymphoblastic Leukemia Adult B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 Adult L1 Acute Lymphoblastic Leukemia Adult L2 Acute Lymphoblastic Leukemia Adult T Acute Lymphoblastic Leukemia Recurrent Adult Acute Lymphoblastic Leukemia Untreated Adult Acute Lymphoblastic Leukemia Collapse <<	Phase 2	Active, not recruiting	September 24, 2019	-
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NCT01190930	Acute Lymphoblastic Leukemia ... more >> Adult B Lymphoblastic Lymphoma Ann Arbor Stage I B Lymphoblastic Lymphoma Ann Arbor Stage II B Lymphoblastic Lymphoma Childhood B Acute Lymphoblastic Leukemia Childhood B Acute Lymphoblastic Leukemia With t(9;22)(q34.1;q11.2); BCR-ABL1 Childhood B Lymphoblastic Lymphoma Down Syndrome Hypodiploid B Acute Lymphoblastic Leukemia Intrachromosomal Amplification of Chromosome 21 Philadelphia Chromosome Positive Untreated Adult Acute Lymphoblastic Leukemia Untreated Childhood Acute Lymphoblastic Leukemia Collapse <<	Phase 3	Active, not recruiting	-	-
NCT02883049	B Acute Lymphoblastic Leukemia... more >> Central Nervous System Leukemia Ph-Like Acute Lymphoblastic Leukemia Testicular Leukemia Untreated Adult Acute Lymphoblastic Leukemia Untreated Childhood Acute Lymphoblastic Leukemia Collapse <<	Phase 3	Recruiting	-	-
NCT02730546	Gastric Cardia Adenocarcinoma ... more >> Gastroesophageal Junction Adenocarcinoma Stage IB Gastric Cancer AJCC v7 Stage II Gastric Cancer AJCC v7 Stage IIA Gastric Cancer AJCC v7 Stage IIB Gastric Cancer AJCC v7 Stage IIIA Gastric Cancer AJCC v7 Stage IIIB Gastric Cancer AJCC v7 Collapse <<	Phase 1 Phase 2	Recruiting	April 15, 2021	United States, Arizona ... more >> Mayo Clinic Hospital Recruiting Phoenix, Arizona, United States, 85054 Contact: Clinical Trials Referral Office 866-776-0015 Principal Investigator: Daniel H. Ahn United States, Minnesota Mayo Clinic Recruiting Rochester, Minnesota, United States, 55905 Contact: Clinical Trials Referral Office 855-776-0015 Principal Investigator: Harry H. Yoon Collapse <<
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NCT00321685	-	-	Active, not recruiting	-	-
NCT02779283	Acute Lymphoblastic Leukemia ... more >> Acute Myeloid Leukemia Collapse <<	Phase 1	Recruiting	June 1, 2019	United States, Oregon ... more >> OHSU Knight Cancer Institute Recruiting Portland, Oregon, United States, 97239 Contact: Stephen E. Spurgeon 503-494-8950 spurgeos@ohsu.edu Principal Investigator: Stephen E. Spurgeon Collapse <<
NCT03007147	B Acute Lymphoblastic Leukemia... more >> BCR-ABL1 Fusion Protein Expression Minimal Residual Disease Philadelphia Chromosome Positive T Acute Lymphoblastic Leukemia Untreated Adult Acute Lymphoblastic Leukemia Untreated Childhood Acute Lymphoblastic Leukemia Collapse <<	Phase 3	Recruiting	June 30, 2026	-
NCT02921256	Rectal Adenocarcinoma ... more >> Stage II Rectal Cancer AJCC v7 Stage III Rectal Cancer AJCC v7 Collapse <<	Phase 2	Recruiting	-	-
NCT02828358	Acute Leukemia of Ambiguous Li... more >>neage Childhood B Acute Lymphoblastic Leukemia KMT2A Gene Rearrangement Mixed Phenotype Acute Leukemia Collapse <<	Phase 2	Suspended(Met accural pending ... more >>evaluation of enrolled pats.) Collapse <<	September 30, 2019	-
NCT00408005	T Acute Lymphoblastic Leukemia... more >> T Lymphoblastic Lymphoma Collapse <<	Phase 3	Completed	-	-
NCT01959672	Pancreatic Adenocarcinoma ... more >> Resectable Pancreatic Carcinoma Stage I Pancreatic Cancer Stage IA Pancreatic Cancer Stage IB Pancreatic Cancer Stage II Pancreatic Cancer Stage IIA Pancreatic Cancer Stage IIB Pancreatic Cancer Stage III Pancreatic Cancer Collapse <<	Phase 2	Active, not recruiting	December 2019	United States, Nebraska ... more >> University of Nebraska Medical Center Omaha, Nebraska, United States, 68198 Collapse <<
NCT02997228	Colorectal Adenocarcinoma ... more >> Mismatch Repair Deficiency Stage IV Colorectal Cancer AJCC v7 Stage IVA Colorectal Cancer AJCC v7 Stage IVB Colorectal Cancer AJCC v7 Collapse <<	Phase 3	Recruiting	April 30, 2022	-
NCT02896907	Pancreatic Adenocarcinoma ... more >> Recurrent Pancreatic Carcinoma Stage III Pancreatic Cancer Stage IV Pancreatic Cancer Unresectable Pancreatic Carcinoma Collapse <<	Early Phase 1	Active, not recruiting	January 1, 2019	United States, Pennsylvania ... more >> Sidney Kimmel Cancer Center at Thomas Jefferson University Philadelphia, Pennsylvania, United States, 19107 Collapse <<
NCT02620865	Metastatic Pancreatic Adenocar... more >>cinoma Recurrent Pancreatic Carcinoma Stage III Pancreatic Cancer Stage IV Pancreatic Cancer Collapse <<	Phase 1 Phase 2	Active, not recruiting	December 2018	United States, Michigan ... more >> Wayne State University/Karmanos Cancer Institute Detroit, Michigan, United States, 48201 Collapse <<
NCT01307956	Adenocarcinoma of the Gastroes... more >>ophageal Junction Esophageal Adenocarcinoma Stage IIA Esophageal Cancer Stage IIB Esophageal Cancer Collapse <<	Phase 2	Terminated(Drug manufacturer -... more >> Amgen requested, per DSMB observation in POWER trial.) Collapse <<	-	United States, Nebraska ... more >> University of Nebraska Medical Center Omaha, Nebraska, United States, 68198 Collapse <<
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NCT03300609	Colorectal Adenocarcinoma ... more >> RAS Wild Type Stage III Colorectal Cancer AJCC v7 Stage IIIA Colorectal Cancer AJCC v7 Stage IIIB Colorectal Cancer AJCC v7 Stage IIIC Colorectal Cancer AJCC v7 Stage IV Colorectal Cancer AJCC v7 Stage IVA Colorectal Cancer AJCC v7 Stage IVB Colorectal Cancer AJCC v7 Collapse <<	Phase 3	Recruiting	February 27, 2023	United States, California ... more >> USC/Norris Comprehensive Cancer Center Recruiting Los Angeles, California, United States, 90033 Contact: Dana Agafitei 323-865-0467 Raluca.Agafitei@med.usc.edu Collapse <<
NCT01307956	-	-	Terminated(Drug manufacturer -... more >> Amgen requested, per DSMB observation in POWER trial.) Collapse <<	-	-
NCT02890355	Metastatic Pancreatic Adenocar... more >>cinoma Recurrent Pancreatic Carcinoma Stage IV Pancreatic Cancer AJCC v6 and v7 Collapse <<	Phase 2	Active, not recruiting	-	-
NCT02912559	Colon Adenocarcinoma ... more >> DNA Repair Disorder Lynch Syndrome Stage III Colon Cancer AJCC v7 Stage IIIA Colon Cancer AJCC v7 Stage IIIB Colon Cancer AJCC v7 Stage IIIC Colon Cancer AJCC v7 Collapse <<	Phase 3	Recruiting	July 1, 2020	-
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NCT02042443	Adult Cholangiocarcinoma ... more >> Advanced Adult Hepatocellular Carcinoma BCLC Stage C Adult Hepatocellular Carcinoma BCLC Stage D Adult Hepatocellular Carcinoma Hilar Cholangiocarcinoma Localized Non-Resectable Adult Liver Carcinoma Recurrent Adult Liver Carcinoma Recurrent Childhood Liver Cancer Recurrent Extrahepatic Bile Duct Carcinoma Recurrent Gallbladder Carcinoma Stage II Gallbladder Cancer Stage III Childhood Hepatocellular Carcinoma Stage IIIA Gallbladder Cancer Stage IIIB Gallbladder Cancer Stage IV Childhood Hepatocellular Carcinoma Stage IV Distal Bile Duct Cancer Stage IVA Gallbladder Cancer Stage IVB Gallbladder Cancer Unresectable Extrahepatic Bile Duct Carcinoma Collapse <<	Phase 2	Completed	-	-
NCT02508077	Recurrent Colorectal Carcinoma... more >> Stage IVA Colorectal Cancer Stage IVB Colorectal Cancer Collapse <<	Phase 2	Terminated(Poor Accrual)	-	United States, California ... more >> City of Hope Medical Center Duarte, California, United States, 91010 City of Hope Antelope Valley Lancaster, California, United States, 93534 City of Hope Rancho Cucamonga Rancho Cucamonga, California, United States, 91730 South Pasadena Cancer Center South Pasadena, California, United States, 91030 Collapse <<
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NCT01383343	Recurrent Colon Carcinoma ... more >> Recurrent Rectal Carcinoma Stage IVA Colon Cancer Stage IVA Rectal Cancer Stage IVB Colon Cancer Stage IVB Rectal Cancer Collapse <<	Phase 1	Completed	-	United States, Arizona ... more >> Mayo Clinic in Arizona Scottsdale, Arizona, United States, 85259 United States, Florida Mayo Clinic in Florida Jacksonville, Florida, United States, 32224-9980 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 Collapse <<
NCT00957905	Recurrent Extragonadal Seminom... more >>a Recurrent Malignant Extragonadal Germ Cell Tumor Recurrent Malignant Extragonadal Non-Seminomatous Germ Cell Tumor Recurrent Malignant Testicular Germ Cell Tumor Recurrent Ovarian Germ Cell Tumor Stage III Testicular Cancer Stage IV Extragonadal Non-Seminomatous Germ Cell Tumor Stage IV Extragonadal Seminoma Stage IV Ovarian Germ Cell Tumor Collapse <<	Phase 2	Completed	-	United States, California ... more >> Tower Cancer Research Foundation Beverly Hills, California, United States, 90211-1850 City of Hope Comprehensive Cancer Center Duarte, California, United States, 91010 USC / Norris Comprehensive Cancer Center Los Angeles, California, United States, 90033 University of California Davis Comprehensive Cancer Center Sacramento, California, United States, 95817 United States, Illinois University of Chicago Comprehensive Cancer Center Chicago, Illinois, United States, 60637 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, New York Memorial Sloan-Kettering Cancer Center New York, New York, United States, 10065 United States, Pennsylvania UPMC-Presbyterian Hospital Pittsburgh, Pennsylvania, United States, 15213 University of Pittsburgh Cancer Institute (UPCI) Pittsburgh, Pennsylvania, United States, 15232 United States, Wisconsin Riverview Hospital Wisconsin Rapids, Wisconsin, United States, 54494 Collapse <<
NCT02508077	-	-	Terminated(Poor Accrual)	-	-
NCT03337087	Biliary System Disorder ... more >> BRCA1 Gene Mutation BRCA2 Gene Mutation Gastroesophageal Junction Adenocarcinoma Homologous Recombination Deficiency Metastatic Pancreatic Adenocarcinoma PALB2 Gene Mutation Stage IV Colorectal Cancer AJCC v7 Stage IV Pancreatic Cancer AJCC v6 and v7 Stage IVA Colorectal Cancer AJCC v7 Stage IVB Colorectal Cancer AJCC v7 Collapse <<	Phase 1 Phase 2	Not yet recruiting	December 31, 2022	United States, Arizona ... more >> Mayo Clinic in Arizona Recruiting Scottsdale, Arizona, United States, 85259 Contact: Clinical Trial Referral Office 855-776-0015 Principal Investigator: Tanios S. Bekaii-Saab United States, Georgia Emory University Hospital/Winship Cancer Institute Not yet recruiting Atlanta, Georgia, United States, 30322 Contact: Christina S. Wu 404-778-0202 christina.wu@emoryhealthcare.org Principal Investigator: Christina S. Wu United States, Minnesota Mayo Clinic Not yet recruiting Rochester, Minnesota, United States, 55905 Contact: Clinical Trials Referral Office 855-776-0015 Principal Investigator: Wen Wee MA United States, Utah Huntsman Cancer Institute/University of Utah Not yet recruiting Salt Lake City, Utah, United States, 84112 Contact: Susan Sharry 801-585-3453 susan.sharry@hci.utah.edu Principal Investigator: Ignacio Garrido-Laguna Collapse <<
NCT00217737	Colon Mucinous Adenocarcinoma ... more >> Colon Signet Ring Cell Adenocarcinoma Lynch Syndrome Stage IIA Colon Cancer AJCC v7 Stage IIB Colon Cancer AJCC v7 Stage IIC Colon Cancer AJCC v7 Collapse <<	Phase 3	Active, not recruiting	-	-
NCT00957905	-	-	Completed	-	-

Folinic acid calcium salt pentahydrate/亚叶酸钙水合物 Catalog No. CSN11049

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