FRAX1036

Product Name: FRAX1036
CAS No.: 1432908-05-8
Chemical Name: FRAX1036
Synonyms: CS-2271;FRAX1036;FRAX-1036;FRAX 1036;FRAX1036 (Free base);FRAX1036, 10 mM in DMSO;FRAX 1036,Inhibitor,p21 activated kinases,PAK,FRAX1036,inhibit,FRAX-1036;6-(2-Chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one;6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-{[2-(1-methylpiperidin-4-yl)ethyl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one;Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-[2-chloro-4-(6-methyl-2-pyrazinyl)phenyl]-8-ethyl-2-[[2-(1-methyl-4-piperidinyl)ethyl]amino]-
CBNumber: CB23122927
Molecular Formula: C28H32ClN7O
Formula Weight: 518.05
MOL File: 1432908-05-8.mol

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FRAX1036 Property

Boiling point:: 669.8±65.0 °C(Predicted)
Density: 1?+-.0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: Soluble in DMSO
form: crystalline solid
pka: 9.46±0.10(Predicted)
color: White to light yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML2618
Product name: FRAX1036
Purity: ≥98% (HPLC)
Packaging: 5 mg
Price: $119.45
Updated: 2025/07/31

Sigma-Aldrich

Product number: SML2618
Product name: FRAX1036
Purity: ≥98% (HPLC)
Packaging: 25 mg
Price: $407
Updated: 2025/07/31

Cayman Chemical

Product number: 20711
Product name: FRAX1036
Purity: ≥98%
Packaging: 1mg
Price: $47
Updated: 2024/03/01

Cayman Chemical

Product number: 20711
Product name: FRAX1036
Purity: ≥98%
Packaging: 5mg
Price: $206
Updated: 2024/03/01

Cayman Chemical

Product number: 20711
Product name: FRAX1036
Purity: ≥98%
Packaging: 10mg
Price: $360
Updated: 2024/03/01

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FRAX1036 Chemical Properties,Usage,Production

Description

FRAX1036 is a selective inhibitor of p21-activated kinase 1 (PAK1), a serine/threonine kinase downstream of Rac1 and Cdc42 that is involved in tumorigenesis. It can induce apoptosis in breast cancer cells and has been shown to potentiate the activity of the microtubule stabilizing agent, docetaxel . Disruption of PAK1 via FRAX1036 has been used to inhibit oncogenic KRAS signaling in non-small cell lung cancer cells.

Uses

FRAX1036 is a PAK inhibitor with Kis of 23.3 nM, 72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4, respectively.

in vitro

previous study demonstrated that the administration of docetaxel with either frax1036 or pak1 small interfering rna oligonucleotides was able to alter signaling to cytoskeletal-associated proteins dramatically, such as stathmin, and also able to induce microtubule disorganization and cellular apoptosis. in addition, the live-cell imaging data showed that the duration of mitotic arrest mediated by docetaxel could be significantly reduced by the treatment of frax1036, which was associated with increased kinetics of apoptosis [1].

in vivo

in previous animal study, the untreated mice bearing kt21 transplants showed ventricular invasion, whereas ben-men grew at the injection site. efficacy results found that the treatment with frax1036 could lead to a slower tumor growth, with reduction in body mass index (bmi) signals of 37% when compared to vehicle cohort [2].

IC 50

PAK1: 23.3 nM (Ki); PAK2: 72.4 nM (Ki); PAK4: 2.4 μM (Ki)

References

[1] ong cc et al. small molecule inhibition of group i p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. breast cancer res.2015 apr 23;17:59.
[2] chow hy et al. group i paks as therapeutic targets in nf2-deficient meningioma. oncotarget.2015 feb 10;6(4):1981-94.

FRAX1036 Preparation Products And Raw materials

Raw materials

Preparation Products

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FRAX1036 Suppliers

China 60 India 1 United States 9 Global 70

Haoyuan Chemexpress Co., Ltd.

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MedChemexpress LLC

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Amadis Chemical Company Limited

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1432908-05-8, FRAX1036Related Search:

FRAX1036

FRAX1036 (Free base)

FRAX-1036;FRAX 1036

CS-2271

Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-[2-chloro-4-(6-methyl-2-pyrazinyl)phenyl]-8-ethyl-2-[[2-(1-methyl-4-piperidinyl)ethyl]amino]-

6-(2-Chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one

FRAX 1036,Inhibitor,p21 activated kinases,PAK,FRAX1036,inhibit,FRAX-1036

6-[2-chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-{[2-(1-methylpiperidin-4-yl)ethyl]amino}-7H,8H-pyrido[2,3-d]pyrimidin-7-one

FRAX1036, 10 mM in DMSO

1432908-05-8

C28H32ClN7O