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

YX-2-107 

Cat. No.: HY-148530
Handling Instructions

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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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].

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

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].

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.
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
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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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.

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Keywords:

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

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