BQU57

Modify Date: 2024-01-02 12:11:28

BQU57 Structure
BQU57 structure
Common Name BQU57
CAS Number 1637739-82-2 Molecular Weight 334.296
Density 1.4±0.1 g/cm3 Boiling Point 493.4±45.0 °C at 760 mmHg
Molecular Formula C16H13F3N4O Melting Point N/A
MSDS USA Flash Point 252.2±28.7 °C

 Use of BQU57


BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth similar to depletion of Ral by siRNA. The IC50 for BQU57 of 2.0 μM in H2122 and 1.3 μM in H358.IC50 value: 2.0 μM (H2122 cell), 1.3 μM (H358 cell)Target: Ralin vitro: BQU57 inhibits Ral binding to its effector RalBP1, Ral-mediated cell spreading in murine fibroblasts and anchorage-independent growth of human cancer cell lines.in vivo: H2122 xenograft tumors are collected 3h after a single intraperitoneal injection BQU57 (10/20/50 mg/kg) and activation of Ral in the extracts is analyzed in RalBP1 pull-down assays. Both RalA and RalB are significantly inhibited by BQU57. By contrast, no inhibition of Ras and RhoA activity is observed.

 Names

Name 6-Amino-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
Synonym More Synonyms

 BQU57 Biological Activity

Description BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth similar to depletion of Ral by siRNA. The IC50 for BQU57 of 2.0 μM in H2122 and 1.3 μM in H358.IC50 value: 2.0 μM (H2122 cell), 1.3 μM (H358 cell)Target: Ralin vitro: BQU57 inhibits Ral binding to its effector RalBP1, Ral-mediated cell spreading in murine fibroblasts and anchorage-independent growth of human cancer cell lines.in vivo: H2122 xenograft tumors are collected 3h after a single intraperitoneal injection BQU57 (10/20/50 mg/kg) and activation of Ral in the extracts is analyzed in RalBP1 pull-down assays. Both RalA and RalB are significantly inhibited by BQU57. By contrast, no inhibition of Ras and RhoA activity is observed.
Related Catalog
References

[1]. Yan C, et al. Discovery and characterization of small molecules that target the GTPase Ral. Nature. 2014 Nov 20;515(7527):443-447.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 493.4±45.0 °C at 760 mmHg
Molecular Formula C16H13F3N4O
Molecular Weight 334.296
Flash Point 252.2±28.7 °C
Exact Mass 334.104156
LogP 2.33
Appearance of Characters white solid
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.610
Storage condition -20℃

 Safety Information

RIDADR NONH for all modes of transport

 Synonyms

MFCD28902198
Pyrano[2,3-c]pyrazole-5-carbonitrile, 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-
6-Amino-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
BQU57
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