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  4. BLU0588

BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research.

For research use only. We do not sell to patients.

BLU0588 Chemical Structure

BLU0588 Chemical Structure

CAS No. : 2810747-78-3

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1 mg USD 230 In-stock
5 mg USD 560 In-stock
10 mg USD 790 In-stock
25 mg USD 1230 In-stock
50 mg USD 1680 In-stock
100 mg USD 2260 In-stock
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Based on 1 publication(s) in Google Scholar

BLU0588 Related Antibodies

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Description

BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research[1].

IC50 & Target

IC50: 1 nM (PRKACA)[1]
In Vitro

BLU0588 (1.5 μM, 1 day or 14 days) reverses a FLC-specific gene signature, leading to downregulation of genes that are overexpressed in FLC (CPS1 and G6PC, top) and upregulation of genes that are underexpressed in FLC[1].
BLU0588 (0-312.5 nM) reduces pVASP in FLC PDX cells in a dose-dependent manner[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BLU0588 Related Antibodies
In Vivo

BLU0588 (30-75 mg/kg, orally, once) can inhibit PRKACA, effectively inhibits downstream signaling of PRKACA, phosphorylated VASP levels returns to baseline levels by 24 hours[1].
The highest tolerated dose of BLU0588 for more than 3 weeks of continuous dosing was established as 30 mg/kg QD in mice[1].
BLU0588 (30 mg/kg, orally, once daily, 34 days) can inhibits tumor growth in mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: female NOD-SCID mice harboring FLC PDX tumors (6-8-week-old, FLC PDX shRNA cell lines or Hep3B cells were implanted)[1]
Dosage: 30 mg/kg
Administration: Orally, once daily, 34 days
Result: Inhibited tumor growth in mice, by day 34 tumor growth was inhibited by 48.5%.
Molecular Weight

423.51

Formula

C26H25N5O
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=CN=C(C2=C3C(NC=C3)=NC=C2)C=C1)N[C@H]4[C@H](N5CCCC5)CC6=CC=CC=C64
Shipping

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

DMSO : 83.33 mg/mL (196.76 mM; ultrasonic and warming and heat to 60°C; 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 2.3612 mL 11.8061 mL 23.6122 mL
5 mM 0.4722 mL 2.3612 mL 4.7224 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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This equation is commonly abbreviated as: C1V1 = C2V2

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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 2.3612 mL 11.8061 mL 23.6122 mL 59.0305 mL
5 mM 0.4722 mL 2.3612 mL 4.7224 mL 11.8061 mL
10 mM 0.2361 mL 1.1806 mL 2.3612 mL 5.9030 mL
15 mM 0.1574 mL 0.7871 mL 1.5741 mL 3.9354 mL
20 mM 0.1181 mL 0.5903 mL 1.1806 mL 2.9515 mL
25 mM 0.0944 mL 0.4722 mL 0.9445 mL 2.3612 mL
30 mM 0.0787 mL 0.3935 mL 0.7871 mL 1.9677 mL
40 mM 0.0590 mL 0.2952 mL 0.5903 mL 1.4758 mL
50 mM 0.0472 mL 0.2361 mL 0.4722 mL 1.1806 mL
60 mM 0.0394 mL 0.1968 mL 0.3935 mL 0.9838 mL
80 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7379 mL
100 mM 0.0236 mL 0.1181 mL 0.2361 mL 0.5903 mL
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BLU0588 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:

BLU05882810747-78-3 BLU 0588BLU-0588PKAProtein kinase AFLC patient-derived xenograftPDXFibrolamellar carcinomaFLC PDX cellsphosphorylated VASPHep3B cellsInhibitorinhibitorinhibit

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