AZD4747

Name: AZD4747
Brand: MedChemExpress
SKU: HY-154959
Rating: 4.5 (0 reviews)

Art. -Nr.: HY-154959 Reinheit: 99.07%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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

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AZD4747 Chemische Struktur

CAS. Nr. : 2489226-14-2

Größe	Verfügbarkeit	Menge
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
Solid
1 mg	Auf Lager	Estimated Time of Arrival: December 31
5 mg	Auf Lager	Estimated Time of Arrival: December 31
10 mg	Auf Lager	Estimated Time of Arrival: December 31
25 mg	Auf Lager	Estimated Time of Arrival: December 31
50 mg	Auf Lager	Estimated Time of Arrival: December 31
100 mg	Auf Lager	Estimated Time of Arrival: December 31
200 mg	Angebot einholen
500 mg	Angebot einholen

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This product is a controlled substance and not for sale in your territory.

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Other Forms of AZD4747:

(9R,12aR)-AZD4747 In-stock

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Ras Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

K-Ras H-Ras N-Ras Ras

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

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].

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.

Molekulargewicht

440.89

Formel

C₂₄H₂₂ClFN₂O₃

CAS. Nr.

2489226-14-2

Appearance

Solid

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

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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.

Molaritätsrechner
Verdünnungsrechner

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Reinheit & Dokumentation

Purity: 99.07%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (258 KB) HNMR (304 KB) LCMS (103 KB)

Handling Instructions (2659 KB)

Verweise

[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]

Complete Stock Solution Preparation Table

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

AZD4747 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:

AZD47472489226-14-2AZD 4747AZD-4747RascancerInhibitorinhibitorinhibit

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AZD4747

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Other Forms of AZD4747:

AZD4747 Related Antibodies

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle Ras Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

AZD4747 Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

Kundenbewertung

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SAFETY DATA SHEET (SDS)

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