PRN1008

Aha kemịkalụ:

(S) -2- (3- (4-amino-3- (2-fluoro-4-phenoxyphenyl)) -1H-pyrazolo [3,4-d] pyrimidin-1-yl) piperidine-1-carbonyl) -4 -methyl-4- (4- (oxetan-3-yl) piperazin-1-yl) pent-2-enenitrile

Koodu Ọchịchọ:

NC1=C2C(N([C@H]3CCCN(C(/C(C#N)=CC(C))(N4CCN(C5COC5)CC4)C)=O)C3)N=C2C6=C(F)C =C(OC7=CC=CC=C7)C=C6=NC=N1

Koodu InChi:

InChi=1S/C36H40FN9O3/c1-36(2,45-15-13-43(14-16-45)26-21-48-22-26)18-24(19-38)35(47)44- 12-6-7-25 (20-44)46-34-31 (33 (39)40-23-41-34)32 (42-46)29-11-10-28 (17-30(29) 37)49-27-8-4-3-5-9-27/h3-5,8-11,17-18,23,25-26H,6-7,12-16,20-22H2,1- 2H3, (H2,39,40,41)/b24-18-/t25-/m0/s1

Igodo InChi:

LCFFREMLXLZNHE-IEUUHXEXSA-N

Okwu:

PRN1008, PRN-1008, PRN 1008,1575596-29-0

Solubility:Soluble na DMSO

Nchekwa:0 - 4 Celsius C maka obere oge (ụbọchị ruo izu), ma ọ bụ -20 Celsius maka ogologo oge (ọnwa).

Nkọwa:

PRN1008 bụ onye na-eme ihe ike, nhọrọ ma na-agbanwe agbanwe nke BTK ((IC50 = 1.3 ± 0.5 nM)) nwere mmetụta PD agbatị na vivo. PRN1008 dị mma yana nnabata nke ọma mgbe ọ gbasịrị otu na ụbọchị iri n'ime mmadụ. Ịme ihe iji nweta> 90% n'ime ya ka a gwọchara ya, na-ebute ọnụnọ na-agbanwe agbanwe na ogologo oge. Mkpuchi ebumnuche BTK nwere ọgwụ kwa ụbọchị nke ≥300mg ruru ọkwa ọgwụgwọ dabere na nyocha ntụgharị n'ụdị oke ọrịa ogbu na nkwonkwo. Nkwado data ndị a na-aga n'ihu na mmepe nke PRN1008 dị ka onye na-ahụ maka ọgwụgwọ maka ọrịa ogbu na nkwonkwo.

Ebumnuche: BTK