[CAS NO. 75607-67-9]  Fludarabinephosphate

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PRODUCTS SPECIFICATIONS [75607-67-9]

Store
Catalog
HY-B0028
Brand
MCE
CAS
75607-67-9

DESCRIPTION [75607-67-9]

Overview

MDLMFCD00866418
Molecular Weight365.21
Molecular FormulaC10H13FN5O7P
SMILESNC1=C2C(N([C@H]3[C@@H](O)[C@H](O)[C@@H](COP(O)(O)=O)O3)C=N2)=NC(F)=N1

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


Summary

Fludarabine (phosphate) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.


In Vitro

Fludarabine phosphate significantly reduces the cell viability in a dose-dependent manner. Fludarabine phosphate exhibits no effect in all tested concentrations when combined with either PBS or control vector, ACE-GFP. Fludarabine phosphate causes a significant decrease in cell viability for 24 h after exposure to ACE-PNP when compared to PBS and ACE-GFP at concentrations of 2.5, 5 and 10 μg/mL [2] .

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


In Vivo

F-araAMP (100 mg/kg given 15 times, 167 mg/kg given 9 times, or 250 mg/kg given 3 times, i.p.) leads to complete regressions of all tumors and cures of all mice. Parental D54 tumors (i.e. without E. coli PNP) are not sensitive to treatment with F-araAMP. Intratumoral injection of Ad/PNP followed by IT F-araAMP can elicit a substantial regressive effect on otherwise refractory solid tumors in a fashion substantially superior to viral PNP transduction followed by systemic prodrug administration [1] . The comparison of ACE-GFP/fludarabine phosphate with ACE-GFP/PBS demonstrats that fludarabine phosphate alone has no growth inhibitory activity on KU-19-19 tumors [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
NCT02024308 Changhai Hospital
Acute Myeloid Leukemia|AML1-ETO Fusion Protein Expression
November 2010 Phase 4
NCT04083170 Fred Hutchinson Cancer Center|National Heart, Lung, and Blood Institute (NHLBI)
Acute Erythroid Leukemia|Acute Lymphoblastic Leukemia|Acute Megakaryoblastic Leukemia|Acute Myeloid Leukemia|Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Hematopoietic and Lymphoid Cell Neoplasm|HIV Infection|Myelodysplastic Syndrome|Myelodysplastic Syndrome With Excess Blasts|Non-Hodgkin Lymphoma|Refractory Anemia
October 6, 2022 Phase 2
NCT03449108 M.D. Anderson Cancer Center|Iovance Biotherapeutics, Inc.|National Cancer Institute (NCI)
Bone Sarcoma|Dedifferentiated Chondrosarcoma|Giant Cell Tumor of Bone|Malignancy in Giant Cell Tumor of Bone|Malignant Solid Neoplasm|Ovarian Carcinosarcoma|Platinum-Resistant Ovarian Carcinoma|Poorly Differentiated Thyroid Gland Carcinoma|Recurrent Osteosarcoma|Recurrent Ovarian Carcinoma|Refractory Osteosarcoma|Soft Tissue Sarcoma|Thyroid Gland Anaplastic Carcinoma|Thyroid Gland Squamous Cell Carcinoma|Undifferentiated High Grade Pleomorphic Sarcoma of Bone|Triple Negative Breast Cancer
April 27, 2018 Phase 2

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:

DMSO : ≥ 100 mg/mL ( 273.82 mM )

H 2 O : 5 mg/mL ( 13.69 mM ; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7382 mL 13.6908 mL 27.3815 mL
5 mM 0.5476 mL 2.7382 mL 5.4763 mL
10 mM 0.2738 mL 1.3691 mL 2.7382 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: phosphate buffer saline

    Solubility: 20 mg/mL (54.76 mM); Clear solution; Need ultrasonic

  • 2.

    Add each solvent one by one: PBS

    Solubility: 18.33 mg/mL (50.19 mM); Clear solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution

  • 4.

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

    Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution

  • 5.

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

    Solubility: ≥ 2.5 mg/mL (6.85 mM); Clear solution

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


Synonyms

9H-Purin-6-amine, 2-fluoro-9-(5-O-phosphono-β-D-arabinofuranosyl)-
2-Fluoro-9-(5-O-phosphono-β-D-arabinofuranosyl)-9H-purin-6-amine
Fludarabine phosphate
NSC 312887
NSC 328002
Fludara
Fludarabine 5′-monophosphate
2-Fluoroadenine arabinoside 5′-monophosphate
FAMP
Fludura
2-F-ara-AMP
Fludarabine 5′-dihydrogen phosphate