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Referencia número: HY-154959

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AZD4747

Name: AZD4747
Brand: MedChemExpress
SKU: HY-154959
Price: 280.00 USD
Availability: InStock
Rating: 5 (1 reviews)

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AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS^G12C inhibitor. AZD4747 has the potential to study cancer.

Para uso exclusivo en investigación. No vendemos a pacientes.

Pureza : 99.07%
No. CAS: 2489226-14-2
Fòrmula: C₂₄H₂₂ClFN₂O₃
Peso molecular:440.89

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

AZD4747 Chemical Structure

No. CAS: 2489226-14-2

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

AZD4747 is a selective, blood-brain barrier-permeable mutant GTPase KRAS^G12C inhibitor. AZD4747 has the potential to study cancer^[1].

IC₅₀ & Target

KRAS^G12C^[1].

Ver todos los productos específicos de isoformas Ras :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	23.31 μM Compound: 14	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay	[PMID: 37395055]
NCI-H358	IC₅₀	0.012 μM Compound: 14	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 3D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo 3D reagent based assay	[PMID: 37395055]
NCI-H358	IC₅₀	0.36 μM Compound: 14	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 2D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo reagent based assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant cultured as 2D spheroids assessed as reduction in cell proliferation incubated for 3 days by CellTiter-Glo reagent based assay	[PMID: 37395055]

In Vivo

AZD4747 (1.1-2.3 μM/kg (i.v.); 2.3-6.8 μM/kg (p.o.); single) shows clearances of moderate to high, with 52 and 75% of hepatic blood flow for the mouse and rat, respectively^[1].

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

Animal Model:

Male CD1 mice, male Wistar Han rats^[1].
Dosage:

Mouse: 2.3 μM/kg (i.v.); 6.8 μM/kg (p.o.);
Rat: 1.1-2.3 μM/kg (i.v.); 6.8 μM/kg (p.o.).
Administration:

i.v. and p.o.
Result:

1.19 Pharmacokinetic Parameters of AZD4747 in Cross Species^[1].

Mouse Rat

IV^a PO^a IV^a PO^a

Eh (%) 52 75

V_ss (L/kg) 2.9 1.7

T_1/2 (h) 0.63 0.56

F% 58 18

Note:
a: 5% DMSO, 95% SBE-B-CD (30% w/v) in water.

Chemical Information

No. CAS 2489226-14-2
Appearance Solid
Peso molecular 440.89
Fòrmula C₂₄H₂₂ClFN₂O₃
Color White to off-white
SMILES

C=CC(N(C[C@@H]1COC2=C3F)CCN1CC2=CC(C#CC)=[C@]3[C@@]4=C(C=CC=C4O)Cl)=O
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvente y solubilidad

In Vitro:

DMSO : 250 mg/mL (567.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2681 mL

11.3407 mL

22.6814 mL

5 mM

0.4536 mL

2.2681 mL

4.5363 mL

10 mM

0.2268 mL

1.1341 mL

2.2681 mL

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.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Kettle JG, et al. Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration. J Med Chem. 2023 Jul 13;66(13):9147-9160. [Content Brief]

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.

Complete Stock Solution Preparation Table

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	2.2681 mL	11.3407 mL	22.6814 mL	56.7035 mL
	5 mM	0.4536 mL	2.2681 mL	4.5363 mL	11.3407 mL
	10 mM	0.2268 mL	1.1341 mL	2.2681 mL	5.6703 mL
	15 mM	0.1512 mL	0.7560 mL	1.5121 mL	3.7802 mL
	20 mM	0.1134 mL	0.5670 mL	1.1341 mL	2.8352 mL
	25 mM	0.0907 mL	0.4536 mL	0.9073 mL	2.2681 mL
	30 mM	0.0756 mL	0.3780 mL	0.7560 mL	1.8901 mL
	40 mM	0.0567 mL	0.2835 mL	0.5670 mL	1.4176 mL
	50 mM	0.0454 mL	0.2268 mL	0.4536 mL	1.1341 mL
	60 mM	0.0378 mL	0.1890 mL	0.3780 mL	0.9451 mL
	80 mM	0.0284 mL	0.1418 mL	0.2835 mL	0.7088 mL
	100 mM	0.0227 mL	0.1134 mL	0.2268 mL	0.5670 mL

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MOQ

Minimum order quantity

100 mg

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vivo
Chemical Information
Solvente y solubilidad
- In Vitro
Pureza y Documentación
Referencias

Nombre del producto:
Referencia número:
Cantidad:
MCE Japan Authorized Agent:

Nombre del producto:
No. CAS:
Species:
Pureza:
Cantidad:

	Mouse		Rat
	IV^a	PO^a	IV^a	PO^a
Eh (%)	52		75
V_ss (L/kg)	2.9		1.7
T_1/2 (h)	0.63		0.56
F%		58		18

AZD4747

Ver todos los productos específicos de isoformas Ras

Actividad biológica

Descripciòn

IC50 & Target

Cellular Effect

In Vivo

Chemical Information

Solvente y solubilidad

In Vitro:

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

AZD4747 Related Classifications

HY-154959 Related Classifications

Bioz

Keywords

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