PHA-848125

Research use only, not for human use.

A potent, selective, brain penetrant and orally available dual CDK and TRK inhibitor with IC50 of 45 and 53 nM for CDK2/cyclin A and TrkA, respectively; shows cross-reactivity with other CDKs (CDK1/4/5/7), TrkB/C, Kit, Abl and PDGFR (IC50s<1 uM).

A potent, selective, brain penetrant and orally available dual CDK and TRK inhibitor with IC50 of 45 and 53 nM for CDK2/cyclin A and TrkA, respectively; shows cross-reactivity with other CDKs (CDK1/4/5/7), TrkB/C, Kit, Abl and PDGFR (IC50s<1 uM); nhibits cell proliferation of a wide panel of tumoral cell lines with submicromolar IC50; shows significant antitumor activity in various human xenografts.Brain Cancer Phase 2 Clinical

Milciclib;PHA 848125

Angiogenesis

CDK

CDK2/CyclinA; CDK4/CyclinD1; CDK5/p35; CDK7/CyclinH; TrkA

Cancer

Brain Cancer

802539-81-7

460.57

C25H32N8O

>98% (HPLC)

10 mM in DMSO

O=C(C1=NN(C)C2=C1C(C)(C)CC3=CN=C(NC4=CC=C(N5CCN(C)CC5)C=C4)N=C23)NC

1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-

(-20℃)

With Ice Pack

≥ 2 years