AZ304 

目录号: HY-117273
产品使用指南

AZ304 是一种 BRAF 双重抑制剂,有效抑制野生型 BRAF,突变型 BRAF (V600E) 和野生型 CRAF,IC50 值分别为 79 nM,38 nM 和 68 nM。AZ304 对其他激酶有显著抑制作用,如 p38 (IC50,6 nM),CSF1R (IC50,35 nM),对 MAP3K7 (IC50,6400 nM) 和 CSK (IC50,7050 nM) 的作用很弱。具有抗肿瘤活性。

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AZ304 Chemical Structure

AZ304 Chemical Structure

CAS No. : 942507-42-8

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥3850 In-stock
5 mg ¥3500 In-stock
10 mg ¥5500 In-stock
50 mg ¥16500 In-stock
100 mg ¥26500 In-stock
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Description

AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM), weak effct on MAP3K7 (IC50, 6400 nM) and CSK (IC50, 7050 nM). Anti-tumor activity[1].

IC50 & Target[1]

BRafV600E

38 nM (IC50)

BRAFWT

79 nM (IC50)

CRAF

68 nM (IC50)

p38

6 nM (IC50)

CSF1R

35 nM (IC50)

MAP3K7

6400 nM (IC50)

CSK

7050 nM (IC50)

In Vitro

AZ304 (1 nM-100 μM) potently reduces ERK phosphorylation (p-ERK), with a mean EC50 of 65 nM in the V600E mutant BRAF containing melanoma cell line A375, and EC50s of 52 nM, 60 nM in the wild type BRAF melanoma cell line SK-MEL-31 with and without EGF[1]. AZ304 also potently inhibits p-p38 in both BRAF genetic statuses cell lines[1].
AZ304 (0, 0.1, 1, 10, 100 μM, 48 and 72 hours) dose-dependently inhibits the growth of RKO, HT-29, DiFi, and Caco-2, with GI50s of 4.539 μM, 3.896 μM, 4.987 μM, 1.763 μM (48 hours) and 0.5032 μM, 0.3887 μM, 0.6354 μM, 0.3772 μM (72 hours), respectively[1].
AZ304 (2 μM, 36 and 48 h) decreases BRAF, p-ERK, p-AKT and p-mTOR levels, increases p-EGFR in both BRAF V600E mutant and BRAF wild type cells. AZ304 down-regulates p-EGFR, inhibits p-ERK, more potently suppresses BRAF, ERK, AKT and mTOR signalling pathways in combination with Cetuximab[1].

Cell Proliferation Assay[1]

Cell Line: RKO, HT-29, DiFi, Caco-2 cells
Concentration: 0, 0.1, 1, 10, 100 μM
Incubation Time: 48, 72 hours
Result: Dose-dependently inhibited the growth of V600E mutant BRAF cell lines (RKO, HT-29) and wild-type BRAF cell lines (DiFi, Caco-2).
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2147 mL 11.0737 mL 22.1474 mL
5 mM 0.4429 mL 2.2147 mL 4.4295 mL
10 mM 0.2215 mL 1.1074 mL 2.2147 mL
*Please refer to the solubility information to select the appropriate solvent.
References
  • [1].

Molecular Weight

451.52

Formula

C₂₇H₂₅N₅O₂

CAS No.

942507-42-8

SMILES

O=C(NC1=CC=C(C)C(NC2=C3C=CC(OC)=CC3=NC=N2)=C1)C4=CC=CC(C(C)(C#N)C)=C4

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

  • [1]。

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产品名称:
AZ304
目录号:
HY-117273
需求量:

AZ304

Cat. No.: HY-117273

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