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YX-2-107

Catalog No. T74710 CAS 2417408-46-7

YX-2-107 is a selective and potent CDK6-degrading PROTAC with an IC50 value of 4.4 nM.YX-2-107 inhibits RB phosphorylation and FOXM1 expression in vitro, and inhibits the development of Ph+ ALL in rats.YX-2-107 can be used for the prophylaxis and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). YX-2-107 can be used for the prevention and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL).

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YX-2-107, CAS 2417408-46-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 226.00
5 mg	In stock	$ 563.00
10 mg	In stock	$ 897.00
25 mg	In stock	$ 1,660.00
50 mg	In stock	$ 2,490.00
100 mg	In stock	$ 3,360.00
1 mL * 10 mM (in DMSO)	In stock	$ 618.00

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Purity: 98.09%

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Description	YX-2-107 is a selective and potent CDK6-degrading PROTAC with an IC50 value of 4.4 nM.YX-2-107 inhibits RB phosphorylation and FOXM1 expression in vitro, and inhibits the development of Ph+ ALL in rats.YX-2-107 can be used for the prophylaxis and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). YX-2-107 can be used for the prevention and treatment of Ph chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL).
Targets&IC50	CDK6:4.4 nM
In vitro	In Ph+ BV173 and SUP-B15 cells, YX-2-107, when applied at a concentration of 2000 nM for 48 hours, demonstrates inhibition of the S phase[1]. Furthermore, at various concentrations (0, 1.6, 8, 40, 200, 1000 nM) for 4 hours, YX-2-107 selectively degrades CDK6 in BV173 cells[1]. Additionally, when used at a concentration of 2000 nM for 72 hours, YX-2-107 inhibits RB phosphorylation and FOXM1 expression in Ph+ BV173 and SUP-B15 cells[1].
In vivo	Following a single intraperitoneal administration at a dose of 10 mg/kg, YX-2-107 achieves a maximum concentration of 741 nM in plasma after 4 hours. This concentration is 150-fold greater than the CDK6 degradation IC50. Clearance from the plasma is observed within the mentioned timeframe[1]. Moreover, when administered at a dose of 150 mg/kg intraperitoneally, once daily for 3 days, YX-2-107 is pharmacologically active in suppressing the proliferation of Ph+ ALL in mice[1].

Molecular Weight	889.95
Formula	C45H51N11O9
CAS No.	2417408-46-7

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (101.13 mM), Sonication is recommended.

References and Literature

1. De Dominici M, et al. Selective inhibition of Ph-positive ALL cell growth through kinase-dependent and -independent effects by CDK6-specific PROTACs. Blood. 2020 Apr 30;135(18):1560-1573.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library

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Keywords

YX-2-107 2417408-46-7 Cell Cycle/Checkpoint CDK inhibitor inhibit

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