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FRAX1036

CAS No.
1432908-05-8
Chemical Name:
FRAX1036
Synonyms
CS-2271;FRAX1036;FRAX-1036;FRAX 1036;FRAX1036 (Free base);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;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
Molecular Weight:
518.05
MDL Number:
MFCD30187513
MOL File:
1432908-05-8.mol
Last updated:2023-07-14 17:42:49

FRAX1036 Properties

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)

FRAX1036 price More Price(24)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 20711 FRAX1036 ≥98% 1432908-05-8 1mg $47 2024-03-01 Buy
Cayman Chemical 20711 FRAX1036 ≥98% 1432908-05-8 5mg $206 2024-03-01 Buy
Cayman Chemical 20711 FRAX1036 ≥98% 1432908-05-8 10mg $360 2024-03-01 Buy
Cayman Chemical 20711 FRAX1036 ≥98% 1432908-05-8 25mg $788 2024-03-01 Buy
AK Scientific 9316DU 6-[2-Chloro-4-(6-methylpyrazin-2-yl)phenyl]-8-ethyl-2-[2-(1-methylpiperidin-4-yl)ethylamino]pyrido[2,3-d]pyrimidin-7-one 1432908-05-8 25mg $974 2021-12-16 Buy
Product number Packaging Price Buy
20711 1mg $47 Buy
20711 5mg $206 Buy
20711 10mg $360 Buy
20711 25mg $788 Buy
9316DU 25mg $974 Buy

FRAX1036 Chemical Properties,Uses,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.

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].

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.

849934-94-7
1432908-05-8
Synthesis of FRAX1036 from Methyl 2-(4-broMo-2-chlorophenyl)acetate

FRAX1036 Preparation Products And Raw materials

Raw materials

Preparation Products

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ATK CHEMICAL COMPANY LIMITED
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Shanghai EFE Biological Technology Co., Ltd. 021-65675885 18964387627 info@efebio.com China 9709 58
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 1432908-05-8 C28H32ClN7O