2. Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  3. Liposome IRE1
  4. G-5758

G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s. G-5758 is well tolerated in multiple myeloma models (KMS-11) at oral doses up to 500 mg/kg in rats. G-5758 exhibits pharmacodynamics comparable to that of induced IRE1 knockdown.

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G-5758 Chemical Structure

G-5758 Chemical Structure

CAS No. : 2413455-99-7

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Description

G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s. G-5758 is well tolerated in multiple myeloma models (KMS-11) at oral doses up to 500 mg/kg in rats. G-5758 exhibits pharmacodynamics comparable to that of induced IRE1 knockdown[1].

Molecular Weight

588.58

Formula

C27H24F4N6O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=C(F)C(NS(CC2=CC=CC=C2)(=O)=O)=C(F)C=C1OC3=C(C=CC=N3)C4=CC=NC(N[C@H]5C[C@H](F)CNC5)=N4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (169.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6990 mL 8.4950 mL 16.9900 mL
5 mM 0.3398 mL 1.6990 mL 3.3980 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6990 mL 8.4950 mL 16.9900 mL 42.4751 mL
5 mM 0.3398 mL 1.6990 mL 3.3980 mL 8.4950 mL
10 mM 0.1699 mL 0.8495 mL 1.6990 mL 4.2475 mL
15 mM 0.1133 mL 0.5663 mL 1.1327 mL 2.8317 mL
20 mM 0.0850 mL 0.4248 mL 0.8495 mL 2.1238 mL
25 mM 0.0680 mL 0.3398 mL 0.6796 mL 1.6990 mL
30 mM 0.0566 mL 0.2832 mL 0.5663 mL 1.4158 mL
40 mM 0.0425 mL 0.2124 mL 0.4248 mL 1.0619 mL
50 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8495 mL
60 mM 0.0283 mL 0.1416 mL 0.2832 mL 0.7079 mL
80 mM 0.0212 mL 0.1062 mL 0.2124 mL 0.5309 mL
100 mM 0.0170 mL 0.0850 mL 0.1699 mL 0.4248 mL
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G-5758 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

G-57582413455-99-7G5758G 5758LiposomeIRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

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