SGI-1776

Research use only, not for human use.

SGI-1776 is a potent, selective, orally active Pim kinase inhibitor with IC50 of 7, 363 and 69 nM for Pim1, Pim2 and Pim3, respectively.

SGI-1776 is a potent, selective, orally active Pim kinase inhibitor with IC50 of 7, 363 and 69 nM for Pim1, Pim2 and Pim3, respectively; exhibits promising selectivity against a panel of >300 kinases, shows inhibitory activity against two other kinases: Flt-3 (IC50=44 nM) and Haspin (IC50=34 nM); reduces cell viability of androgen-independent prostate cancer cell lines with IC50 of 2-4 uM, causes cell cycle arrest and caspase-dependent apoptosis in prostate cancer cells, marginally sensitizes prostate cancer cells to taxane-based therapeutics by inhibiting MDR1 activity and inducing apoptosis; shows efficacy in xenograft model bearing MV-4-11 tumors.Prostate Cancer Phase 1 Clinical.

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SGI 1776 | SGI1776

JAK/STAT Signaling

Pim

FLT3|Pim1|Pim2|Pim3

Cancer

Prostate Cancer

1025065-69-3

405.42

C20H22F3N5O

>98% (HPLC)

10 mM in DMSO

FC(F)(F)OC1=CC=C(C2=CN=C3C=CC(NCC4CCN(C)CC4)=NN32)C=C1

Imidazo[1,2-b]pyridazin-6-amine, N-[(1-methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-

(-20℃)

With Ice Pack

≥ 2 years