化合物FRAX597

Name	FRAX597
Synonyms	FRAX597 CS-1774 FRAX 597 FRAX-597 6-(2-chloro-4-(thiazol-5-yl)phenyl)-8-ethyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrido[2,3-d]pyrimidin-7(8H)-one 6-[2-Chloro-4-(5-thiazolyl)phenyl]-8-ethyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]pyrido[2,3-d]pyrimidin-7(8H)-one 6-(2-Chloro-4-thiazol-5-yl-phenyl)-8-ethyl-2-[4-(4-Methyl-piperazin-1-yl)-phenylaMino]-8H-pyrido[2,3-d]pyriMidin-7-one Pyrido[2,3-d]pyriMidin-7(8H)-one, 6-[2-chloro-4-(5-thiazolyl)phenyl]-8-ethyl-2-[[4-(4-Methyl-1-piperazinyl)phenyl]aMino]-
CAS	1286739-19-2

Molecular Formula	C29H28ClN7OS
Molar Mass	558.1
Melting Point	>220°C (dec.)
Solubility	10 mM in DMSO
Appearance	Solid
Color	Yellow
Storage Condition	Refrigerator
In vitro study	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 study	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.

Last Update：2024-01-02 23:10:35

biological activity	FRAX597 is a potent, ATP-competitive first-class inhibitor of PAKs for PAK1,PAK2, and PAK3 have an IC50 of 8 nM,13 nM, and 19 nM, respectively.
in vitro study	FRAX597 (100 n M) displays a significant inhibition capacity toward YES1 (87 %), RET (82 %), CSF1R (91 %), TEK (87 %), PAK1 (82 %), and PAK2 (93 %), while Events Management Index activity the group II: pakks (7 %), PAK6) (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 studies	In NOD/SCID mice which bearing Nf2-/-SC4 Schwann cells, FRAX 597 (100 mg/kg/day, p.o.) causes more significant tumor growth inhibition. 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.
Target	PAK1 8 nM (IC 50 ) PAK2 13 nM (IC 50 ) PAK3 19 nM (IC 50 )

Last Update：2024-04-09 21:11:58

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CAS: 1286739-19-2
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Product Name: FRAX597 Visit Supplier Webpage Request for quotation
CAS: 1286739-19-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

Wechat: 18301782025

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化合物FRAX597

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