N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide

Product Name: N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
CAS No.: 702676-93-5
Chemical Name: N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide
Synonyms: BX320;BX-320 (BX320);N'-[3-[[5-bromo-2-[3-(pyrrolidine-1-carbonylamino)anilino]pyrimidin-4-yl]amino]propyl]-2,2-dimethylpropanediamide;N1-[3-[[5-Bromo-2-[[3-[(1-pyrrolidinylcarbonyl)amino]phenyl]amino]-4-pyrimidinyl]amino]propyl]-2,2-dimethylpropanediamide;N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide;Propanediamide, N1-[3-[[5-bromo-2-[[3-[(1-pyrrolidinylcarbonyl)amino]phenyl]amino]-4-pyrimidinyl]amino]propyl]-2,2-dimethyl-
CBNumber: CB32500501
Molecular Formula: C23H31BrN8O3
Formula Weight: 547.44804
MOL File: 702676-93-5.mol

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N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide Property

storage temp.: -20°C
solubility: DMSO: soluble
form: A crystalline solid
color: White to off-white

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Hazard and Precautionary Statements (GHS)

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N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide Chemical Properties,Usage,Production

Uses

BX-320 is a selective, ATP-competitive, orally acitive, and direct PDK1 inhibitor with an IC50 of 30 nM in a direct kinase assay format. BX-320 also induces apoptosis. Anticancer effect[1].

in vivo

BX-320 (oral dosing with 200 mg/kg, twice a day for 21 days) shows efficacy in a blood-borne metastasis model. BX-320 inhibits the growth of LOX melanoma tumors in the lungs of nude mice after injection of tumor cells into the tail vein. BX-320 has efficacy in an in vivo tumor model, which may reflect an inhibition of productive implantation of tumor cells in the lung or an inhibition of subsequent tumor growth^[1].

Animal Model:	Athymic (nu/nu) female mice, 6-8 weeks old^[1]
Dosage:	200 mg/kg; dose volume was 10 mL/kg
Administration:	Oral gavage twice daily (12 h apart)
Result:	Significantly inhibited the growth of lung tumors in this model.

References

[1] Richard I Feldman, et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. DOI:10.1074/jbc.M501367200

N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide Preparation Products And Raw materials

Raw materials

Preparation Products

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N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide Suppliers

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702676-93-5, N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamideRelated Search:

N1-[3-[[5-Bromo-2-[[3-[(1-pyrrolidinylcarbonyl)amino]phenyl]amino]-4-pyrimidinyl]amino]propyl]-2,2-dimethylpropanediamide

N'-[3-[[5-bromo-2-[3-(pyrrolidine-1-carbonylamino)anilino]pyrimidin-4-yl]amino]propyl]-2,2-dimethylpropanediamide

N-(3-(4-(3-(3-Amino-2,2-dimethyl-3-oxopropanamido)propylamino)-5-bromopyrimidin-2-ylamino)phenyl)pyrrolidine-1-carboxamide

BX320

BX-320 (BX320)

Propanediamide, N1-[3-[[5-bromo-2-[[3-[(1-pyrrolidinylcarbonyl)amino]phenyl]amino]-4-pyrimidinyl]amino]propyl]-2,2-dimethyl-

702676-93-5

C23H31BrN8O3