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).

For research use only. We do not sell to patients.

YX-2-107 Chemical Structure

YX-2-107 Chemical Structure

CAS No. : 2417408-46-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 748 In-stock
Solution
10 mM * 1 mL in DMSO USD 748 In-stock
Solid
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10 mg USD 1080 In-stock
25 mg USD 2000 In-stock
50 mg USD 3000 In-stock
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Based on 1 publication(s) in Google Scholar

YX-2-107 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

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)

In Vitro

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 Related Antibodies

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.
In Vivo

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
Molecular Weight

889.95

Formula

C45H51N11O9
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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
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)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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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mg/kg

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
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Tween-80 +
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Saline
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.
Purity & Documentation
References

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

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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