CAS 209799-67-7|Forodesine

Introduction：Basic information about CAS 209799-67-7|Forodesine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Forodesine BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	Forodesine
CAS Number	209799-67-7	Molecular Weight	266.25300
Density	2.01	Boiling Point	613.5ºC at 760mmHg
Molecular Formula	C₁₁H₁₄N₄O₄	Melting Point	/
MSDS	/	Flash Point	324.8ºC

Names

Name	immucillin H
Synonym	More Synonyms

Forodesine BiologicalActivity

Description	Forodesine(BCX-1777 freebase; Immucillin-H) is an orally bioavailable PNP inhibitor with picomolar potency; induces apoptosis, mainly in T cells.IC50 value:Target: PNP inhibitorForodesine and ara-G cytotoxicities were higher in T-cell acute lymphoblastic leukemia (T-ALL) samples than in B-cell precursor (BCP)-ALL and acute myeloid leukemia (AML) samples. Resistance to forodesine did not preclude ara-G sensitivity and vice versa, indicating that both drugs rely on different resistance mechanisms [1]. BCX1777 was well tolerated at doses up to 300 mg once daily and showed preliminary evidence of activity in relapsed or refractory peripheral T/natural killer-cell malignancies, warranting further investigation [2]. after 48 hours of treatment with forodesine there was a slight dGTP increase in 5T33MM and RPMI-8226 MM cells associated with partial inhibition of proliferation and a limited induction of apoptosis [3]. In the presence of 10 μM deoxyguanosine, forodesine effectively inhibited the growth of CEM cells but not that of CEM/ara-G cells [4].
Related Catalog	Signaling Pathways >>Cell Cycle/DNA Damage >>Nucleoside Antimetabolite/AnalogResearch Areas >>Cancer
References	[1]. Homminga I, et al. In vitro efficacy of forodesine and nelarabine (ara-G) in pediatric leukemia. Blood. 2011 Aug 25;118(8):2184-90. [2]. Ogura M, et al. Phase I study of BCX1777 (forodesine) in patients with relapsed or refractory peripheral T/natural killer-cell malignancies. Cancer Sci. 2012 Jul;103(7):1290-5. [3]. Bieghs L, et al. The effects of forodesine in murine and human multiple myeloma cells. Adv Hematol. 2010;2010:131895. [4]. Yamauchi T, et al. A nelarabine-resistant T-lymphoblastic leukemia CCRF-CEM variant cell line is cross-resistant to the purine nucleoside phosphorylase inhibitor forodesine. Anticancer Res. 2014 Sep;34(9):4885-92.

Description

Forodesine(BCX-1777 freebase; Immucillin-H) is an orally bioavailable PNP inhibitor with picomolar potency; induces apoptosis, mainly in T cells.IC50 value:Target: PNP inhibitorForodesine and ara-G cytotoxicities were higher in T-cell acute lymphoblastic leukemia (T-ALL) samples than in B-cell precursor (BCP)-ALL and acute myeloid leukemia (AML) samples. Resistance to forodesine did not preclude ara-G sensitivity and vice versa, indicating that both drugs rely on different resistance mechanisms [1]. BCX1777 was well tolerated at doses up to 300 mg once daily and showed preliminary evidence of activity in relapsed or refractory peripheral T/natural killer-cell malignancies, warranting further investigation [2]. after 48 hours of treatment with forodesine there was a slight dGTP increase in 5T33MM and RPMI-8226 MM cells associated with partial inhibition of proliferation and a limited induction of apoptosis [3]. In the presence of 10 μM deoxyguanosine, forodesine effectively inhibited the growth of CEM cells but not that of CEM/ara-G cells [4].

Related Catalog

Signaling Pathways >>Cell Cycle/DNA Damage >>Nucleoside Antimetabolite/AnalogResearch Areas >>Cancer

References

[1]. Homminga I, et al. In vitro efficacy of forodesine and nelarabine (ara-G) in pediatric leukemia. Blood. 2011 Aug 25;118(8):2184-90.

[2]. Ogura M, et al. Phase I study of BCX1777 (forodesine) in patients with relapsed or refractory peripheral T/natural killer-cell malignancies. Cancer Sci. 2012 Jul;103(7):1290-5.

[3]. Bieghs L, et al. The effects of forodesine in murine and human multiple myeloma cells. Adv Hematol. 2010;2010:131895.

[4]. Yamauchi T, et al. A nelarabine-resistant T-lymphoblastic leukemia CCRF-CEM variant cell line is cross-resistant to the purine nucleoside phosphorylase inhibitor forodesine. Anticancer Res. 2014 Sep;34(9):4885-92.

Chemical & Physical Properties

Density	2.01
Boiling Point	613.5ºC at 760mmHg
Molecular Formula	C₁₁H₁₄N₄O₄
Molecular Weight	266.25300
Flash Point	324.8ºC
Exact Mass	266.10200
PSA	134.26000
Vapour Pressure	6.61E-16mmHg at 25°C
Index of Refraction	1.894
InChIKey	IWKXDMQDITUYRK-KUBHLMPHSA-N
SMILES	O=c1[nH]cnc2c(C3NC(CO)C(O)C3O)c[nH]c12

Synonyms

Isopamphos

Fodosine

Immucillin-H

Forodesine

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