1. Cell Cycle/DNA Damage Apoptosis
  2. DNA/RNA Synthesis Apoptosis
  3. BOLD-100

BOLD-100  (Synonyms: NKP-1339; IT-139; KP-1339)

製品番号: HY-16350 純度: 95.20%
COA 取扱説明書 Technical Support

BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

BOLD-100

BOLD-100 構造式

CAS 番号 : 197723-00-5

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 210 在庫あり
Solution
10 mM * 1 mL in DMSO USD 210 在庫あり
Solid
5 mg $190 在庫あり
10 mg $285 在庫あり
25 mg $520 在庫あり
50 mg $770 在庫あり
100 mg $1155 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of BOLD-100:

Top Publications Citing Use of Products

DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示:

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

BOLD-100 (NKP-1339; IT-139) is the first-in-class ruthenium-based anticancer agent in development against solid cancer with limited side effects. BOLD-100 induces G2/M cell cycle arrest, blockage of DNA synthesis, and induction of apoptosis via the mitochondrial pathway. BOLD-100 has a high tumor targeting potential, strongly binds to serum proteins such as albumin and transferrin and activates in the reductive tumor milieu[1].

体外実験

BOLD-100 (0-200 μM; 72 hours) has the anticancer activity against malignant cell lines of diverse origin, exhibits IC50 values of 45-200 μM for KP1339 mono-therapy. It against Hepatoma cell line, Hep3B, HepG2, PLC/PRF/5 and HCC2 cells with the Mean IC50 value of 186.3 μM, 165.4 μM, 124.4 μM, and 69.4 μM, respectively. It against Melanoma cell line, VM-1, VM-21,VM-48 with IC50 values of 178 μM, 111 μM, and 143 μM, respectively. It against Lung cancer and Colon cancer cell lines, inhibits A549, VL-8, SW480 and HCT116 cells, respectively[2].
BOLD-100 (0-150 μM; 24 hours) induces cell apoptosis alone. When it combines with sorafenib, it increases the numbers of the apopotic cells. Additionally, the p-PARP and caspase 7 cleavage is promoted either[2].
BOLD-100 (0-150 μM; 24 hours) can promote phosphorylation of STAT3 and CREB expression, however, the decreasation is inhibited by sorafenib cotreatment[2].

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

Cell Viability Assay[2]

Cell Line: Hepatoma, Melanoma, Lung cancer and Colon cancer cell lines
Concentration: 0 μM, 50 μM, 100 μM, 150 μM and 200 μM
Incubation Time: 72 hours
Result: Has anti-cancer activity in diverse malignant tumour cell types.

Apoptosis Analysis[2]

Cell Line: Hep3B cells
Concentration: 0 μM, 75 μM, 150 μM
Incubation Time: 72 hours
Result: Promoted cell apoptosis as a concentration manner.

Western Blot Analysis[2]

Cell Line: Hep3B cells
Concentration: 0 μM, 75 μM, 150 μM
Incubation Time: 72 hours
Result: Increased p-STAT3 and p-CREB expression in cells without sorafenib cotreatment.
体内実験

BOLD-100 (intravenous injection; 30 mg/kg; once a week; 42sdays) combines with the multi-kinase inhibitor sorafenib and exhibits a further anticancer activity when compares to the BOLD-100 treatment alone in Hep3B xenografts grown in Balb/c SCID mice [2].

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

Animal Model: Hep3B xenograft in Balb/c mice[2]
Dosage: 30 mg/kg
Administration: Intravenous injection
Result: Had synergistic activity of KP1339 with sorafenib in vivo.
分子量

502.14

分子式

C14H12Cl4N4NaRu

CAS 番号
Appearance

Solid

Color

Brown to dark brown

SMILES

[Cl-][Ru+3]([Cl-])([Cl-])([N]1=CC2=C(N1)C=CC=C2)([N]3=CC4=C(N3)C=CC=C4)[Cl-].[Na+]

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度
体外: 

DMSO : ≥ 59 mg/mL (117.50 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9915 mL 9.9574 mL 19.9148 mL
5 mM 0.3983 mL 1.9915 mL 3.9830 mL
10 mM 0.1991 mL 0.9957 mL 1.9915 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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)

C1

×
体積 (開始)

V1

=
濃度 (終了)

C2

×
体積 (終了)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
純度とドキュメンテーション
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 (sealed storage, away from moisture). 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 1.9915 mL 9.9574 mL 19.9148 mL 49.7869 mL
5 mM 0.3983 mL 1.9915 mL 3.9830 mL 9.9574 mL
10 mM 0.1991 mL 0.9957 mL 1.9915 mL 4.9787 mL
15 mM 0.1328 mL 0.6638 mL 1.3277 mL 3.3191 mL
20 mM 0.0996 mL 0.4979 mL 0.9957 mL 2.4893 mL
25 mM 0.0797 mL 0.3983 mL 0.7966 mL 1.9915 mL
30 mM 0.0664 mL 0.3319 mL 0.6638 mL 1.6596 mL
40 mM 0.0498 mL 0.2489 mL 0.4979 mL 1.2447 mL
50 mM 0.0398 mL 0.1991 mL 0.3983 mL 0.9957 mL
60 mM 0.0332 mL 0.1660 mL 0.3319 mL 0.8298 mL
80 mM 0.0249 mL 0.1245 mL 0.2489 mL 0.6223 mL
100 mM 0.0199 mL 0.0996 mL 0.1991 mL 0.4979 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

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.

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

 

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

     

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
BOLD-100
製品番号:
HY-16350
数量:
MCE 日本正規代理店: