4-Amino-5,6,7,8-tetrahydro-5-oxo-8-(β-D-ribofuranosyl)pyrido[2,3-d]pyrimidine-6-carboxamide

Product Name4-Amino-5,6,7,8-tetrahydro-5-oxo-8-(β-D-ribofuranosyl)pyrido[2,3-d]pyrimidine-6-carboxamide
CAS36707-00-3
MFC13H15N5O6
MW337.29
EINECS
MOL File36707-00-3.mol

Chemical Properties

Boiling point	795.771±60.00 °C(Press: 760.00 Torr)(predicted)
Density	1.792±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
storage temp.	Store at RT
solubility	DMF: slightly soluble; DMSO: 2 mg/ml
form	powder
pka	12.077±0.20(predicted)
color	white to beige
InChI	1S/C13H15N5O6/c14-10-6-7(20)4(11(15)23)1-18(12(6)17-3-16-10)13-9(22)8(21)5(2-19)24-13/h1,3,5,8-9,13,19,21-22H,2H2,(H2,15,23)(H2,14,16,17)/t5-,8-,9-,13-/m1/s1
InChIKey	SPBWHPXCWJLQRU-FITJORAGSA-N
SMILES	O=C1C(C(N)=O)=CN([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)C3=C1C(N)=NC=N3

Safety Information

RIDADR	UN 2811 6.1 / PGIII
WGK Germany	WGK 3
Storage Class	6.1C - Combustible acute toxic Cat.3 toxic compounds or compounds which causing chronic effects
Hazard Classifications	Acute Tox. 3 Oral

Usage And Synthesis

Uses

NSC 177223 is a Akt/protein kinase B inhibitor. It binds to pleckstrin homologous domain of Akt and blocks Akt membrane translocation. Treatment of cancer cells with NSC 177223 results in inhibition of the kinase activities and induction of cell growth arrest and apoptosis selectively in human cancer cells that harbor constitutively activated Akt.

Biological Activity

API-1 is a potent and specific Akt/PKB inhibitor. API-1 binds to pleckstrin homology (PH) domain of Akt and blocks Akt membrane translocation. The compound inhibits all three members of the family Akt1/PKBa, Akt2/PKBb and Akt3/PKBg. API-1 does not inhibit the activation of PKC, SGK, PKA, STAT3, Erk-1/2 or JNK.

in vivo

API-1 (10 mg/kg; i.p.; daily for 6-8 weeks) selectively inhibits the growth of tumors with hyperactivated Akt in OVCAR3 and PANC-1 xenograft mice model^[3].

Animal Model:	8-week-old female nude mice (implanted tumors with hyperactivated Akt (OVCAR3 and PANC-1) into the left flank and those tumors that express low levels of activated Akt (OVCAR5 and COLO357) into the right flank)^[3]
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection (i.p.); daily for 6-8 weeks
Result:	Inhibited OVCAR3 and PANC1 tumor growth by 70 and 50%, respectively. Had little effect on the growth of OVCAR5 and COLO357 cells in nude mice. Had no effects on blood glucose level, body weight, activity, and food intake of mice. Phosphorylation levels of Akt were reduced about 70% without a change of total Akt content.

IC 50

Caspase-8; Caspase 3; Caspase-9; PARP

storage

Store at RT

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