2. PROTAC Cell Cycle/DNA Damage
  3. PROTACs CDK
  4. YX-2-107

YX-2-107 is a PROTAC (IC50= 4.4 nM) that selectively degrades CDK6. YX-2-107 effectively inhibits RB phosphorylation and FOXM1 expression in vitro and inhibits the development of Ph+ ALL in rats. YX-2-107 can be used in the study of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL).

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YX-2-107

YX-2-107 構造式

CAS 番号 : 2417408-46-7

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 1331 在庫あり
Solution
10 mM * 1 mL in DMSO USD 1331 在庫あり
Solid
1 mg $272 在庫あり
5 mg $680 在庫あり
10 mg $1080 在庫あり
25 mg $2000 在庫あり
50 mg $3000 在庫あり
100 mg $4200 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

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YX-2-107 関連抗体

Top Publications Citing Use of Products

PROTACs 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
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

CDK 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
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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製品説明

YX-2-107 is a PROTAC (IC50= 4.4 nM) that selectively degrades CDK6. YX-2-107 effectively inhibits RB phosphorylation and FOXM1 expression in vitro and inhibits the development of Ph+ ALL in rats. YX-2-107 can be used in the study of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL)[1].

IC50 & Target[1]

CDK6

4.4 nM (IC50)

体外実験

YX-2-107 (2000 nM; 48 h) shows inhibition of S phase in Ph+ BV173 and SUP-B15 cells[1].
YX-2-107 (0, 1.6, 8, 40, 200, 1000 nM;4 h) selectively degrades CDK6 in BV173 cells[1].
YX-2-107 (2000 nM; 72 h) inhibits RB phosphorylation and FOXM1 expression in Ph+ BV173 and SUP-B15 cells[1].

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

YX-2-107 関連抗体

Cell Cycle Analysis[1]

Cell Line: Ph+ BV173 and SUP-B15 cells
Concentration: 2000 nM
Incubation Time: 48 h
Result: Inhibited S-phase entry.

Western Blot Analysis[1]

Cell Line: Ph+ BV173 and SUP-B15 cells
Concentration: 2000 nM
Incubation Time: 72 h
Result: Inhibited the phosphorylation of RB and the expression of FOXM1.
体内実験

YX-2-107 (10 mg/kg; i.p.; single) shows a maximum concentration of 741 nM (150-fold greater than CDK6 degradation IC50), with clearance from the plasma after 4 hours[1].
YX-2-107 (150 mg/kg; i.p.; single daily for 3 days) is pharmacologically active in suppressing Ph+ ALL proliferation in mice[1].

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

Animal Model: NRG-SGM3 mice (Ph+ ALL xenografts model)[1].
Dosage: 150 mg/kg
Administration: Intraperitoneal injection; single daily for 3 days
Result: Suppressed the percentage of primary Ph+ ALL S-phase cells, the expression of CDK4/6-regulated phospho-RB and, to a lesser degree, FOXM1, and induced the selective CDK6 degradation.
Animal Model: C57BL/6j mice[1].
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; single
Result: 1.19 Pharmacokinetic Parameters of YX-2-107 in C57BL/6j mice [1].
IP (10 mg/kg)
Tmax (h) 0.5
Cmax (ng/mL) 660
AUC0-t (ng/mL·h) 815
AUC0-∞ (ng/mL·h) 987
分子量

889.95

分子式

C45H51N11O9
CAS 番号
Appearance

Solid

Color

Yellow to orange

SMILES

O=C1NC(C(CC1)N2C(C3=C(C2=O)C(OCC(NCCCCNCC(N4CCN(CC4)C5=CN=C(NC6=NC(N(C7CCCC7)C(C(C(C)=O)=C8C)=O)=C8C=N6)C=C5)=O)=O)=CC=C3)=O)=O
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 : 100 mg/mL (112.37 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 1.1237 mL 5.6183 mL 11.2366 mL
5 mM 0.2247 mL 1.1237 mL 2.2473 mL
10 mM 0.1124 mL 0.5618 mL 1.1237 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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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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

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体積 （開始）

V1

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C2

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V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (2.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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+
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 98.60%

COA (246 KB) HNMR (216 KB) LCMS (95 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 1.1237 mL 5.6183 mL 11.2366 mL 28.0915 mL
5 mM 0.2247 mL 1.1237 mL 2.2473 mL 5.6183 mL
10 mM 0.1124 mL 0.5618 mL 1.1237 mL 2.8091 mL
15 mM 0.0749 mL 0.3746 mL 0.7491 mL 1.8728 mL
20 mM 0.0562 mL 0.2809 mL 0.5618 mL 1.4046 mL
25 mM 0.0449 mL 0.2247 mL 0.4495 mL 1.1237 mL
30 mM 0.0375 mL 0.1873 mL 0.3746 mL 0.9364 mL
40 mM 0.0281 mL 0.1405 mL 0.2809 mL 0.7023 mL
50 mM 0.0225 mL 0.1124 mL 0.2247 mL 0.5618 mL
60 mM 0.0187 mL 0.0936 mL 0.1873 mL 0.4682 mL
80 mM 0.0140 mL 0.0702 mL 0.1405 mL 0.3511 mL
100 mM 0.0112 mL 0.0562 mL 0.1124 mL 0.2809 mL
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YX-2-107 Related Classifications

  • 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.

Keywords:

YX-2-1072417408-46-7PROTACsCDKCyclin dependent kinaseacute lymphoblastic leukemiaALLPh+BV173 cellSUP-B15 cellFOXM1Inhibitorinhibitorinhibit

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