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FRAX 597

FRAX597

CAS: 1286739-19-2

Molecular Formula: C29H28ClN7OS

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FRAX 597 - Names and Identifiers

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

FRAX 597 - Physico-chemical Properties

Molecular FormulaC29H28ClN7OS
Molar Mass558.1
Melting Point>220°C (dec.)
Solubility 10 mM in DMSO
AppearanceSolid
ColorYellow
Storage ConditionRefrigerator
In vitro studyFRAX597 (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 studyIn 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.

FRAX 597 - Preparation solution concentration reference

 1mg5mg10mg
1 mM1.792 ml8.959 ml17.918 ml
5 mM0.358 ml1.792 ml3.584 ml
10 mM0.179 ml0.896 ml1.792 ml
5 mM0.036 ml0.179 ml0.358 ml
Last Update:2024-01-02 23:10:35

FRAX 597 - Reference Information

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
FRAX 597
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Shanghai Amole Biotechnology Co., Ltd.
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Shanghai Yuanye Bio-Technology Co., Ltd.
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CAS: 1286739-19-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
Shanghai Amole Biotechnology Co., Ltd.
Spot supply
Product Name: FRAX597 Request for quotation
CAS: 1286739-19-2
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
Shanghai Macklin Biochemical Co., Ltd
Spot supply
Product Name: FRAX597 Visit Supplier Webpage Request for quotation
CAS: 1286739-19-2
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: FRAX597 Visit Supplier Webpage Request for quotation
CAS: 1286739-19-2
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Spot supply
Product Name: FRAX597 Visit Supplier Webpage Request for quotation
CAS: 1286739-19-2
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
Shanghai Yuanye Bio-Technology Co., Ltd.
Product Name: FRAX597 Visit Supplier Webpage Request for quotation
CAS: 1286739-19-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
View History
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