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[CAS NO. 53910-25-1] Pentostatin

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Catalog:	HY-A0006
Brand:	MCE
CAS:	53910-25-1

Overview

MDL	MFCD00078802
Molecular Weight	268.27
Molecular Formula	C11H16N4O4
SMILES	O[C@H]1C(N=CN2[C@H](O[C@@H]3CO)C[C@@H]3O)=C2NC=NC1

For research use only. We do not sell to patients.

7 Publications Citing Use of MCE

[1]Sci Transl Med. 2020 May 6;12(542):eaba0769.
[2]Neurobiol Stress. 2021 Sep 11;15:100396.
[3]J Nanobiotechnology. 2019 Mar 29;17(1):45.
[4]PLoS Pathog. 2020 Mar 16;16(3):e1008341.
[5]Virulence. 2018;9(1):1509-1520.
[6]J Immunol. 2022 Jul 1;ji2200142.
[7]J Neurochem. 2019 Aug;150(3):282-295.

Summary

Pentostatin (CI-825; Deoxycoformycin) is an irreversible inhibitor of adenosine deaminase with K _i of 2.5 pM.

IC50 & Target

Ki: 2.5 pM (adenosine deaminase)

In Vivo

In ECP and Pentostatin (CI-825; Deoxycoformycin; 4 mg/m ² , i.v.) treatment, all dogs develop granulocytopenia with <500 granulocytes/μL from day 4. Thrombocytopenia (<20,000 platelets/μL) occurs from day 7 after HCT with nadirs of 3000 to 14000 platelets/μL ^[1] . Pentostatin (2 mg/kg) in combination with cordycepin (2 mg/kg) is 100% effective in the T. evansi-infected mice. There is an increase in levels of some biochemical parameters, especially on liver enzymes, which are accompanied by histological lesions in the liver and kidneys. Pentostatin individually has no curative effect on infected groups ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00144430	Ann & Robert H Lurie Children´s Hospital of Chicago\|Astex Pharmaceuticals, Inc.	Graft vs Host Disease	January 2004	Phase 2
NCT00003005	Boston Medical Center\|National Cancer Institute (NCI)	Leukemia	December 1997	Phase 1
NCT00453193	M.D. Anderson Cancer Center\|Astex Pharmaceuticals, Inc.\|Bayer	Lymphoma\|Leukemia	September 2004	Phase 2
NCT01059786	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Hairy Cell Leukemia	July 1, 2010	Phase 2
NCT00496340	H. Lee Moffitt Cancer Center and Research Institute	Hematologic Malignancies	July 2007	Phase 2
NCT02105766	National Heart, Lung, and Blood Institute (NHLBI)\|National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Sickle Cell Disease\|Thalassemia\|Stem Cell Transplantation\|Graft vs Host Disease	April 21, 2014	Phase 2
NCT00923845	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Renal Cell Carcinoma\|Graft-Versus-Host Disease\|Engraftment Syndrome	March 1, 2008	Phase 2
NCT00038025	M.D. Anderson Cancer Center	Peripheral T-cell Lymphoma\|Cutaneous T-cell Lymphoma\|Chronic Lymphocytic Leukemia	September 6, 1994	Phase 2
NCT01024010	Mayo Clinic\|National Cancer Institute (NCI)	Chronic Lymphocytic Leukemia\|Stage 0 Chronic Lymphocytic Leukemia\|Stage I Chronic Lymphocytic Leukemia\|Stage I Small Lymphocytic Lymphoma\|Stage II Chronic Lymphocytic Leukemia\|Stage II Small Lymphocytic Lymphoma\|Stage III Chronic Lymphocytic Leukemia\|Stage III Small Lymphocytic Lymphoma\|Stage IV Chronic Lymphocytic Leukemia\|Stage IV Small Lymphocytic Lymphoma	March 2010	Phase 2
NCT00816413	University of Nebraska\|National Cancer Institute (NCI)	Chronic Myeloproliferative Disorders\|Leukemia\|Lymphoma\|Myelodysplastic Syndromes\|Nonmalignant Neoplasm	September 2008	Phase 1\|Phase 2
NCT00402714	Yale University\|Hospira, now a wholly owned subsidiary of Pfizer	Hematologic Malignancies	July 2006	Phase 2
NCT00096161	Fred Hutchinson Cancer Center\|National Cancer Institute (NCI)	Acute Lymphoblastic Leukemia\|Acute Myeloid Leukemia\|Chronic Lymphocytic Leukemia\|Chronic Myelogenous Leukemia, BCR-ABL1 Positive\|Graft Versus Host Disease\|Hodgkin Lymphoma\|Myelodysplastic+Myeloproliferative Neoplasm\|Non-Hodgkin Lymphoma\|Plasma Cell Myeloma\|Waldenstrom Macroglobulinemia	May 2003	Phase 2
NCT00254163	US Oncology Research\|Astex Pharmaceuticals, Inc.	B-Cell Chronic Lymphocytic Leukemia	December 2003	Phase 3
NCT03077542	National Heart, Lung, and Blood Institute (NHLBI)\|National Institutes of Health Clinical Center (CC)	Sickle Cell Disease	April 6, 2017	Phase 1\|Phase 2
NCT00049413	Hoag Memorial Hospital Presbyterian\|Cancer Biotherapy Research Group	Leukemia\|Lymphoma	June 2002	Phase 2
NCT00816595	Mayo Clinic\|National Cancer Institute (NCI)	Leukemia\|Lymphoma	February 2009	Phase 2
NCT01188798	St. Jude Children´s Research Hospital	Acute Lymphoblastic Leukemia\|Acute Myelocytic Leukemia\|Chronic Myelocytic Leukemia\|Hodgkin´s Disease\|Myelodysplastic Syndrome	September 2010	Phase 3
NCT00057954	Eastern Cooperative Oncology Group\|National Cancer Institute (NCI)	Lymphoma	June 2005	Phase 2
NCT00224874	National Heart, Lung, and Blood Institute (NHLBI)\|National Cancer Institute (NCI)\|Blood and Marrow Transplant Clinical Trials Network	Graft vs Host Disease\|Immune System Disorders	September 2005	Phase 2
NCT00201721	Ohio State University Comprehensive Cancer Center\|Astex Pharmaceuticals, Inc.	B-Chronic Lymphocytic Leukemia	July 2002	Phase 2
NCT01362790	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Mesothelioma\|Adenocarcinoma of Lung\|Pancreatic Neoplasms	May 11, 2011	Phase 1\|Phase 2
NCT01681563	Niguarda Hospital\|Regione Lombardia\|GlaxoSmithKline\|Hospira, now a wholly owned subsidiary of Pfizer	Chronic Lymphocytic Leukemia	September 2011	Phase 2
NCT00045305	Eastern Cooperative Oncology Group\|National Cancer Institute (NCI)	Leukemia\|Myelodysplastic Syndromes\|Myelodysplastic+Myeloproliferative Neoplasms	May 2005	Phase 2
NCT00074282	Eastern Cooperative Oncology Group\|National Cancer Institute (NCI)	Leukemia	December 16, 2004	Phase 2
NCT00026351	Pharmatech Oncology\|National Cancer Institute (NCI)	Leukemia\|Lymphoma	December 2000	Phase 2
NCT00006968	Jonsson Comprehensive Cancer Center\|National Cancer Institute (NCI)	Kidney Cancer	September 2000	Phase 1\|Phase 2
NCT00003658	Memorial Sloan Kettering Cancer Center\|National Cancer Institute (NCI)	Leukemia\|Lymphoma	September 1998	Phase 2
NCT00541034	Memorial Sloan Kettering Cancer Center\|National Cancer Institute (NCI)\|Astex Pharmaceuticals, Inc.	Leukemia\|Lymphoma	May 2005	Phase 2
NCT00201786	Ohio State University Comprehensive Cancer Center	Graft-Versus-Host Disease	July 2003	Phase 2
NCT00709215	OncoVista, Inc.\|AAIPharma	Refractory TdT-Positive Leukemia	June 2008	Phase 1\|Phase 2
NCT03249831	City of Hope Medical Center\|California Institute for Regenerative Medicine (CIRM)	Sickle Cell Disease\|Sickle Cell Disorder\|Hemoglobinopathies\|Thalassemia\|Anemia, Sickle Cell	January 4, 2019	Phase 1
NCT00506922	M.D. Anderson Cancer Center\|Astex Pharmaceuticals, Inc.	Leukemia\|Lymphoma	September 2000	Phase 1\|Phase 2
NCT00032773	Astex Pharmaceuticals, Inc.	Acute Graft Versus Host Disease	January 30, 2002	Phase 1\|Phase 2
NCT00669318	Mayo Clinic\|National Cancer Institute (NCI)	Leukemia\|Lymphoma	July 2008	Phase 2
NCT01352312	Sidney Kimmel Cancer Center at Thomas Jefferson University\|GlaxoSmithKline\|Novartis\|Thomas Jefferson University	Chronic Lymphocytic Leukemia\|B-Cell Non-Hodgkin´s Lymphoma	May 25, 2011	Phase 1
NCT00602836	Mayo Clinic\|National Cancer Institute (NCI)	Leukemia\|Lymphoma	February 2008	Phase 2
NCT00546377	Memorial Sloan Kettering Cancer Center\|National Cancer Institute (NCI)	Leukemia\|Lymphoma	July 2005	Phase 1\|Phase 2
NCT00571662	University of Nebraska\|Astex Pharmaceuticals, Inc.	Acute Myelogenous Leukemia\|Acute Lymphocytic Leukemia\|Chronic Myelogenous Leukemia\|Chronic Lymphocytic Leukemia\|Myelodysplastic Syndromes\|Multiple Myeloma\|Non-Hodgkins Lymphoma\|Hodgkins Disease\|Peripheral T-cell Lymphoma	December 2000	Phase 2
NCT00074035	Alliance for Clinical Trials in Oncology\|National Cancer Institute (NCI)	Graft Versus Host Disease	December 2003	Phase 2
NCT00698685	University of Arizona\|National Cancer Institute (NCI)	Leukemia\|Lymphoma\|Hodgkin´s Disease\|Hematologic Neoplasms\|Multiple Myeloma\|Carcinoma, Renal Cell	January 23, 2006	Phase 2
NCT03112603	Incyte Corporation	Graft-versus-host Disease (GVHD)	March 7, 2018	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

H ₂ O : 100 mg/mL ( 372.76 mM ; Need ultrasonic)

DMSO : ≥ 50 mg/mL ( 186.38 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.7276 mL	18.6379 mL	37.2759 mL
5 mM	0.7455 mL	3.7276 mL	7.4552 mL
10 mM	0.3728 mL	1.8638 mL	3.7276 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (7.75 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (7.75 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.08 mg/mL (7.75 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Bethge WA, et al. Extracorporeal photopheresis combined with pentostatin in the conditioning regimen for canine hematopoietic cell transplantation does not prevent GVHD. Bone Marrow Transplant. 2014 Sep;49(9):1198-204.
[2] Dalla Rosa L, et al. Cordycepin (3'-deoxyadenosine) pentostatin (deoxycoformycin) combination treatment of mice experimentally infected with Trypanosoma evansi. Parasitology. 2013 Apr;140(5):663-71.

Synonyms

Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-β-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (8R)-

Imidazo[4,5-d][1,3]diazepin-8-ol, 3-(2-deoxy-β-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydro-, (R)-

(8R)-3-(2-Deoxy-β-D-erythro-pentofuranosyl)-3,4,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol

CL 67310465

2′-Deoxycoformycin

NSC 218321

Co-Vidarabine

Pentostatin

Deoxycoformycin

Cl 825

Nipent

Deaminase inhibitor

2′-DCF

Vira A deaminase inhibitor

CI 825

PD-ADI

Co-V

2′-Dexoycoformycin

NSC 247520

Coforin

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