| 產品描述 | |
| 描述 |
FRAX597 is a small molecule inhibitor of the p21-activated kinases, inhibits tumorigenesis of neurofibromatosis type 2 (NF2)-associated Schwannomas. |
| 純度 |
>98%
|
| 儲存/保存方法 |
store at -20℃ for one year（Powder）；
in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. |
| 基本信息 | |
| 別名 |
FRAX 597；FRAX-597；FRAX597
|
| 外觀 |
Powder
|
| 可溶性/溶解性 |
DMSO ：14 mg/mL warmed (25.08 mM)
|
| 生物活性 | |
| 靶點 |
PAK1,PAK2,PAK2,PAK3
|
| In vitro(體外研究) |
FRAX597 (100 n M) displays a significant inhibitory capacity toward YES1 (87%), RET (82%), CSF1R (91%), TEK (87%), PAK1 (82%), and PAK2 (93%), while displays minimal inhibitory activity towards the group II PAKs: PAK4 (0%), PAK6 (23%), and PAK7 (8%). FRAX597 treatment dramatically impairs the proliferation of Nf2-null SC4 Schwann cells (SC4 cells). FRAX597 displays an IC50 value of 48 nM against wild type PAK1, while IC 50 values against the V342F and V342Y PAK1 mutants are higher than 3μM and 2 μM, respectively. FRAX597 inhibits the proliferation and motility of both benign (Ben-Men1, 3μM) and malignant (KT21-MG1, 0.4 μM) meningiomas cells after treating of 72 h.
|
| In vivo(體內研究) |
In NOD/SCID mice which bearing Nf2-/-SC4 Schwann cells, FRAX597 (100 mg/kg/day, p.o.) causes more significant tumor growth inhibition cpmpared with control mice. In SCID mice with orthotopic meningioma, FRAX597 (90 mg/kg/day, p.o.) significantly suppresses tumor growth. In KrasG12D mice, treatment with FRAX597 (90 mg/kg/day, p.o.) causes tumor regression and loss of Erk and Akt activity.
|
FRAX597
- Identification
Reaxys ID: 23567473 Chemical Names: FRAX597, FRAX-597 CAS Registry Number(s): 1286739-19-2 Molecular Formula: C29H28ClN7OS Linear Structure Formula: C29H28ClN7OS Molecular Weight: 558.107 No of references: 9 InChIKey: DHUJCQOUWQMVCG-UHFFFAOYSA-N
