ChemicalBook > CAS DataBase List > 903564-48-7

903564-48-7

Product Name: 903564-48-7
CAS No.: 903564-48-7
Chemical Name: 903564-48-7
Synonyms: UM-164;CS-2793;DAS-DFGO-II;UM-164 ，S8706;UM164;UM-164;UM 164;UM-164 (DAS-DFGO-II);UM-164 trifluoroacetate salt;p38 MAPK,Autophagy,UM-164,Src,UM 164,inhibit,Inhibitor;2-((6-(4-(2-Hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)thiazole-5-carboxamide;2-[[6-[4-(2-Hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-5-thiazolecarboxamide
CBNumber: CB54033656
Molecular Formula: C30H31F3N8O3S
Formula Weight: 640.68
MOL File: 903564-48-7.mol

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903564-48-7 Property

Density: 1.433±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: DMSO: 5 mg/ml
form: A crystalline solid
pka: 11.40±0.70(Predicted)
color: White to off-white
Water Solubility: H2O: 10mg/mL, clear

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML1928
Product name: UM-164 trifluoroacetate salt
Purity: ≥98% (HPLC)
Packaging: 5 mg
Price: $93.19
Updated: 2025/07/31

Cayman Chemical

Product number: 26188
Product name: UM-164
Packaging: 1mg
Price: $44
Updated: 2024/03/01

Cayman Chemical

Product number: 26188
Product name: UM-164
Packaging: 5mg
Price: $140
Updated: 2024/03/01

Cayman Chemical

Product number: 26188
Product name: UM-164
Packaging: 10mg
Price: $257
Updated: 2024/03/01

Cayman Chemical

Product number: 26188
Product name: UM-164
Packaging: 25mg
Price: $533
Updated: 2024/03/01

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903564-48-7 Chemical Properties,Usage,Production

Uses

UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.

Biological Activity

UM-164 (DAS-DFGO-II) is a potent c-Src inhibitor with Kd of 2.7 nM. It also highly inhibits p38α and p38β activity.

in vitro

In biochemical assays, UM-164 is a highly potent inhibitor of c-Src with a binding constant comparable with Dasatinib (UM-164 K _d =2.7 nM, Dasatinib K _d =0.7 nM). To confirm that UM-164 is capable of inhibiting the activation of c-Src in vitro, the effect of UM-164 is examined on the c-Src autophosphorylation in two TNBC cell lines ( MDA-MB 231 and SUM 149). Inhibition of c-Src autophosphorylation is detected in a concentration- and a time-dependent manner. At 120 minutes, complete abrogation of c-Src autophosphorylation is observed at 50 nM, demonstrating that UM-164 is a potent c-Src inhibitor in vitro. Flow cytometry experiments demonstrate that UM-164 treatment of MDA-MB 231 and SUM 149 increased the proportion of G ₀ -G ₁ cells by 25% and 28%, respectively, and concurrently decreased the fraction of S cells by 16% and 19%, respectively.

in vivo

A xenograft study is performed using NCr/nude mice implanted with MDA-MB 231 and SUM 149 cell lines. Once the tumors become palpable, the mice are randomized into control and treatment groups. Mice are injected intraperitoneally with either drug (10 and 20 mg/kg in both xenograft studies; a 15 mg/kg dose is added to the SUM 149 xenograft studies) or vehicle every other day (n=5 for each group). At the selected doses of UM-164 , there is no significant weight loss or gross abnormalities observed in the treated animals, even after 52 days of treatment. However, tumor growth is significantly inhibited in both the 10 mg/kg and 20 mg/kg dose groups compared with the vehicle-treated group (P<0.026 and P<0.004, respectively).

target

p38α

p38β

c-Src

2.7 nM (Kd)

IC 50

c-Src: 2.7 nM (Kd); p38α; p38β

References

[1] Gilani RA, et al. UM-164: A Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer. Clin Cancer Res. 2016 Oct 15;22(20):5087-5096. DOI:10.1158/1078-0432.CCR-15-2158

903564-48-7 Preparation Products And Raw materials

Raw materials

Preparation Products

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903564-48-7, 903564-48-7Related Search:

UM-164

DAS-DFGO-II

CS-2793

UM164;UM-164;UM 164

UM-164 (DAS-DFGO-II)

5-Thiazolecarboxamide, 2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-

p38 MAPK,Autophagy,UM-164,Src,UM 164,inhibit,Inhibitor

2-((6-(4-(2-Hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)thiazole-5-carboxamide

UM-164 trifluoroacetate salt

2-[[6-[4-(2-Hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-5-thiazolecarboxamide

UM-164 ，S8706

903564-48-7

C30H31F3N8O3S