DATASHEET
Formulation
Powder
Storage:
Store in dry, dark place at -20C for 1 year.
Product Information:
Molecular Weight: 500.6
Formula: C27 H32 N8 O2
CAS Number: 955365-80-7
InChi Key: BKWJAKQVGHWELA-UHFFFAOYSA-N
InChi: InChI=1S/C27H32N8O2/c1-5-13-34-25(36)21-18-28-26(29-19-9-11-20(12-10-19)33-16-14-32(4)15-17-33)31-24(21)35(34)23-8-6-7-22(30-23)27(2,3)37/h5-12,18,37H,1,13-17H2,2-4H3,(H,28,29,31)
Smiles: CN1CCN(CC1)C1C=CC(=CC=1)NC1N=C2C(=CN=1)C(=O)N(CC=C)N2C1C=CC=C(N=1)C(C)(C)O
Purity: 98.0
Solubility: DMSO up to 100 mM
Appearance: Solid Power.
Shelf Life: 1.0 years
Description:
MK-1775 (AZD1775) is a highly potent, selective and orally bioavailable Wee1 kinase inhibitor with IC50 of 5.2 nM. It abrogated DNA damaged checkpoints induced by gemcitabine, carboplatin, and cisplatin etc. and enhanced the anti-tumor efficacy of these agents selectively in p53-deficient tumor cells. At tolerated doses, MK-1775 treatment leads to xenograft tumor growth inhibition or regression. It inhibits Wee1 in H3K36me3-deficient cells results in RRM2 reduction, critical dNTP depletion, S-phase arrest, and apoptosis. MK-1775 can regresse H3K36me3-deficient tumor xenografts too. Right now MK-1775 is in phase I/II clinical trials for various cancers.