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Art. -Nr.: HY-131312

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Crelosidenib

Name: Crelosidenib
Brand: MedChemExpress
SKU: HY-131312
Price: 990.00 USD
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(Synonyms: LY3410738; Mutant IDH1-IN-6)

Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC₅₀s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.

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CAS. Nr.: 2230263-60-0
Formel: C₂₈H₃₆N₆O₃
Molecular Weight:504.62

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

Crelosidenib Chemical Structure

CAS. Nr.: 2230263-60-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IDH1

IDH2

Alle Isocitrate Dehydrogenase (IDH) Isoform-spezifische Produkte anzeigen :

IDH1
IDH2

In Vitro

Mutant IDH1-IN-6 (example 2) inhibits production of 2-hydroxyglutarate in HT1080 cells with an IC50 of 1.28 nM, indicating the inhibition of mutant IDHl R132C in cells. aKG, a metabolite generated by wild-type IDHl is not affected by Mutant IDH1-IN-6, indicating Mutant IDH1-IN-6 is selective for mutant IDHl over wild type IDHl in cells^[1].

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

In Vivo

Mutant IDH1-IN-6 (Example 2; 0-32 mg/kg; oral gavage; twice daily; for 3 days) treatment inhibitis of 2-hydroxyglutarate in a dose-dependent manner in IDHl mutant xenograft mice^[1].

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

Animal Model:

Athymic nude mice (20-22 g) injected with TB08 cells^[1]
Dosage:

1 mg/kg, 2 mg/kg, 4 mg/kg, 8 mg/kg, 16 mg/kg, 32 mg/kg
Administration:

Oral gavage; twice daily; for 3 days
Result:

Inhibitied of 2-hydroxyglutarate in IDHl mutant xenograft mice.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2230263-60-0
Molecular Weight 504.62
Formel C₂₈H₃₆N₆O₃
SMILES

O=C1OCC2=CN=C(N[C@H](C3=CC=C([C@@H](N4CCN(C(C=C)=O)CC4)CC5CC5)C=C3)C)N=C2N1CC
Synonyms

LY3410738; Mutant IDH1-IN-6
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Renato Alejandro BAUER, et al. 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors. WO2018111707A1.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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