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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $226 | In Stock | |
5 mg | $563 | In Stock | |
10 mg | $897 | In Stock | |
25 mg | $1,660 | In Stock | |
50 mg | $2,490 | In Stock | |
100 mg | $3,360 | In Stock | |
1 mL x 10 mM (in DMSO) | $618 | In Stock |
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). |
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 |
Storage | keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90 mg/mL (101.13 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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