2. MAPK/ERK Pathway NF-κB Apoptosis
  3. p38 MAPK JNK NF-κB MDM-2/p53
  4. Darizmetinib

Darizmetinib  (Synonyms: HRX-0215)

製品番号: HY-152860 純度: 99.94%
COA 取扱説明書 Technical Support

Darizmetinib (HRX-0215) is an orally active, potent and selective inhibitor of mitogen-activated protein kinase kinase 4 (MKK4). Darizmetinib leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration. Darizmetinib is promising for research of preventing liver failure after extensive oncological liver resections or transplantation of small liver grafts.

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Darizmetinib

Darizmetinib 構造式

CAS 番号 : 2369583-33-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 196 在庫あり
Solution
10 mM * 1 mL in DMSO USD 196 在庫あり
Solid
5 mg $195 在庫あり
10 mg $304 在庫あり
25 mg $495 在庫あり
50 mg $690 在庫あり
100 mg $970 在庫あり
250 mg $1460 在庫あり
500 mg $2100 在庫あり
1 g $2950 在庫あり
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Darizmetinib 関連抗体

Top Publications Citing Use of Products

p38 MAPK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

JNK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
JNK1 JNK2 JNK3 JNK

NF-κB アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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製品説明

Darizmetinib (HRX-0215) is an orally active, potent and selective inhibitor of mitogen-activated protein kinase kinase 4 (MKK4). Darizmetinib leads to enhancement of the MKK7 and JNK1 signaling pathways, thereby activating the transcription factors ATF2 and ELK1, promoting cell proliferation and liver regeneration. Darizmetinib is promising for research of preventing liver failure after extensive oncological liver resections or transplantation of small liver grafts[1][2][3].

体外実験

Darizmetinib (0.3, 1,3 μM, 2 h) reduces lipopolysaccharide (LPS) (HY-D1056)-induced pMKK4 levels in peripheral blood mononuclear cells (PBMCs)[3].

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

Darizmetinib 関連抗体

Western Blot Analysis[3]

Cell Line: PBMCs
Concentration: 0.3, 1,3 μM
Incubation Time: 2 h
Result: Reduced pMKK4 levels in a potent and dose-dependent manner in PBMCs, confirming cell membrane permeability.
体内実験

Darizmetinib (30 mg/kg, p.o., a single dose for 15 min-24 h) increases the number of proliferating hepatocytes upon partial hepatectomy in fibrotic mouse livers [3].
Darizmetinib (10 mg/kg, p.o., a single dose for 2 h and 9 h) activates pro-regenerative program by increaseing MKK7 and JNK1 signaling with a downstream activation of the transcription factors ATF2 and ELK1, reduces p38- and p53 activation, activates nuclear factor κB (NF-κB) signaling, and upregulates the anti-apoptotic protein Bcl-XL in hepatectomized mice[3].
Darizmetinib (5 mg/kg, i.v., every 12 h, starting 24 h before surgery)--mediated suppression of MKK4 increases hepatocyte regeneration in a pig hepatectomy model[3].

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

Animal Model: partial hepatectomy in fibrotic mouse livers[2]
Dosage: 30 mg/kg
Administration: p.o., a single dose for 15 min-24 h
Result: Enhanced hepatocyte proliferation in partial hepatectomy in fibrotic mouse livers, suggesting that the presence of fibrosis per se does not interfere with the Darizmetinib-mediated pro-regenerative mechanism.
分子量

457.45

分子式

C21H17F2N5O3S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C(NS(=O)(CCC)=O)=C1F)F)C2=NNC3=NC=C(C4=CC=NC=C4)C=C32
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 175 mg/mL (382.56 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 2.1860 mL 10.9302 mL 21.8603 mL
5 mM 0.4372 mL 2.1860 mL 4.3721 mL
10 mM 0.2186 mL 1.0930 mL 2.1860 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.

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純度とドキュメンテーション

純度: 99.94%

COA (250 KB) HNMR (290 KB) LCMS (93 KB)

取扱説明書 (2659 KB)
参考文献

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1860 mL 10.9302 mL 21.8603 mL 54.6508 mL
5 mM 0.4372 mL 2.1860 mL 4.3721 mL 10.9302 mL
10 mM 0.2186 mL 1.0930 mL 2.1860 mL 5.4651 mL
15 mM 0.1457 mL 0.7287 mL 1.4574 mL 3.6434 mL
20 mM 0.1093 mL 0.5465 mL 1.0930 mL 2.7325 mL
25 mM 0.0874 mL 0.4372 mL 0.8744 mL 2.1860 mL
30 mM 0.0729 mL 0.3643 mL 0.7287 mL 1.8217 mL
40 mM 0.0547 mL 0.2733 mL 0.5465 mL 1.3663 mL
50 mM 0.0437 mL 0.2186 mL 0.4372 mL 1.0930 mL
60 mM 0.0364 mL 0.1822 mL 0.3643 mL 0.9108 mL
80 mM 0.0273 mL 0.1366 mL 0.2733 mL 0.6831 mL
100 mM 0.0219 mL 0.1093 mL 0.2186 mL 0.5465 mL
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Darizmetinib Related Classifications

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The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Darizmetinib2369583-33-3HRX-0215HRX0215HRX 0215p38 MAPKJNKNF-κBMDM-2/p53c-Jun N-terminal kinaseNuclear factor-κBNuclear factor-kappaBorally activeMKK4MKK7JNK1ATF2ELK1liver failureInhibitorinhibitorinhibit

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