China (Mainland)
1429881-91-3 in bulk supply 1429881-91-3 on hot selling Offer 1429881-91-3 UNC2025 CAS NO.1429881-91-3
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- Min.Order: 1 Gram
- Payment Terms: T/T,MoneyGram,Other
- Available Specifications:
99%(1-5)Gram98%(1-5)Gram
- Product Details
Keywords
- 1429881-91-3 in bulk supply
- 1429881-91-3 on hot selling
- Offer 1429881-91-3 UNC2025
Quick Details
- ProName: 1429881-91-3 in bulk supply 1429881-91...
- CasNo: 1429881-91-3
- Molecular Formula: C28H40N6O
- Appearance: Powder
- Application: Scientific research
- DeliveryTime: Prompt
- PackAge: As required
- Port: Shanghai
- ProductionCapacity: 1000 Gram/Week
- Purity: 98%
- Storage: keep sealed and keep from direct light
- Transportation: By Sea/Air/FedEx
- LimitNum: 1 Gram
- Moisture Content: N/A
- Impurity: N/A
- Grade: Industrial Grade，Pharma Grade
Superiority
1429881-91-3 in bulk supply on hot selling Offer UNC2025
UNC-2025 is a novel potent and highly orally bioavailable Mer/FLT3 dual inhibitor, capable of inhibiting Mer phosphorylation in vivo, following oral dosing as demonstrated by pharmaco-dynamic (PD) studies examining phospho-Mer in leukemic blasts from mouse bone marrow. Kinome profiling versus more than 300 kinases in vitro and cellular selectivity assessments demonstrate that UNC-2025 has similar subnanomolar activity against Flt3, an additional important target in acute myelogenous leukemia (AML), with pharmacologically useful selectivity versus other kinases examined.
UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia.
Details
UNC2025 is a potent, orally bioavailable inhibitor of the tyrosine kinases Mer and Flt3 (IC50s = 0.74 and 0.80 nM, respectively).It less potently inhibits Axl and Tyro3 (IC50s = 14 and 17 nM, respectively) and a panel of related kinases. UNC2025 blocks colony formation of Mer- and Flt3-dependent tumor cell lines and inhibits Mer phosphorylation in bone marrow leukemia cells in vivo. Pharmacokinetic studies suggest that orally administered UNC2025 at 3 mg/kg will suffice to provide 90% inhibition of Mer and Flt3 at 30 min.
| Identification | ||||
| Name | trans-4-[2-(Butylamino)-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]cyclohexanol | |||
| Synonyms | UNC 2025 | |||
| Molecular Structure | ||||
| Molecular Formula | C28H40N6O | |||
| Molecular Weight | 476.66 | |||
| CAS Registry Number | 1429881-91-3 | |||
| Properties | ||||
| Solubility | Insuluble (1.3E-3 g/L) (25 ºC), Calc.* | |||
| Density | 1.24±0.1 g/cm3 (20 ºC 760 Torr), Calc.* | |||
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