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Cat. No.: HY-154959

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AZD4747

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

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

Purity: 99.07%
CAS No.: 2489226-14-2
Formula: C₂₄H₂₂ClFN₂O₃
Molecular Weight:440.89

Storage:

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

AZD4747 Chemical Structure

CAS No.: 2489226-14-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

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].

All Ras Isoforms :

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

CAS No. 2489226-14-2
Appearance Solid
Molecular Weight 440.89
Formula 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
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 : 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.

Molarity Calculator

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

Mass Mass

Concentration Concentration

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Molecular Weight Molecular Weight

Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Handling Instructions (2659 KB)

References

[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

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

	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

MCE Bioactive Compound Library

All Ras Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

AZD4747 Related Classifications

Cat. No.: HY-154959