Methanone, (2,6-dimethyl-4-pyridinyl)[4-[7-(trans-4-hydroxycyclohexyl)-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-1-piperidinyl]-
![Methanone, (2,6-dimethyl-4-pyridinyl)[4-[7-(trans-4-hydroxycyclohexyl)-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-1-piperidinyl]- Structure](CAS/20210305/GIF/2226789-82-6.gif)
- CAS No.
- 2226789-82-6
- Chemical Name:
- Methanone, (2,6-dimethyl-4-pyridinyl)[4-[7-(trans-4-hydroxycyclohexyl)-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-1-piperidinyl]-
- Synonyms
- UNC5293;Methanone, (2,6-dimethyl-4-pyridinyl)[4-[7-(trans-4-hydroxycyclohexyl)-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-1-piperidinyl]-
- CBNumber:
- CB39280396
- Molecular Formula:
- C30H42N6O2
- Molecular Weight:
- 518.69
- MDL Number:
- MOL File:
- 2226789-82-6.mol
Methanone, (2,6-dimethyl-4-pyridinyl)[4-[7-(trans-4-hydroxycyclohexyl)-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-1-piperidinyl]- Properties
| Boiling point | 742.2±70.0 °C(Predicted) |
|---|---|
| Density | 1.28±0.1 g/cm3(Predicted) |
| storage temp. | 4°C, protect from light |
| solubility | DMSO : 100 mg/mL (192.79 mM; Need ultrasonic) |
| pka | 14?+-.0.40(Predicted) |
| form | Viscous Liquid |
| color | Colorless to light yellow |
Methanone, (2,6-dimethyl-4-pyridinyl)[4-[7-(trans-4-hydroxycyclohexyl)-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-1-piperidinyl]- Chemical Properties,Uses,Production
Biological Activity
UNC5293 is a MERTK-selective and potent inhibitor (Ki=190 pM). UNC5293 inhibits MERTK (IC50=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research[1]. UNC5293 provides selective target inhibition in cell-based assays. In cultures of the human B-cell acute lymphoblastic leukemia (B-ALL) cell line, UNC5293 inhibits phosphorylation of MERTK with an IC50 of 9.4 nM. In the SEM B-ALL cell line, UNC5293 is less potent against FLT3, with an IC50 of 170 nM[1]. UNC5293 (oral administration; 120 mg/kg; single dose) effectively inhibit MERTK in vivo in orthotopic 697 B-ALL mice xenografts[1].UNC5293 (oral gavage; 3 mg/kg; single dose) has excellent mouse PK properties (7.8 h half-life and 58% oral bioavailability), and the Cmax and AUClast are 9.2 μM and 2.5 h*μM, respectively[1].
References
[1]. Hongchao Zheng, et al. UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem. 2021 May 17;220:113534.
Methanone, (2,6-dimethyl-4-pyridinyl)[4-[7-(trans-4-hydroxycyclohexyl)-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-1-piperidinyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
Methanone, (2,6-dimethyl-4-pyridinyl)[4-[7-(trans-4-hydroxycyclohexyl)-2-[[(1S)-1-methylbutyl]amino]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-1-piperidinyl]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd. | 17702719238 17702719238 | sales@sun-shinechem.com | China | 972 | 64 |
| Shanghai Chaolan Chemical Technology Center | 021-QQ：65489617 15618227136 | Sales@ATKchemical.com | China | 7268 | 58 |
| Dezhou LonWel Pharmaceutical Technology Co., Ltd. | 13761310616 | 39324283@qq.com | China | 1991 | 58 |
| TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24647 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11974 | 58 |
| Shanghai?Medlife?Pharm-Tech?Co.,?Ltd | 021-59167510 18117107507 | vip@med-life.cn | China | 4997 | 58 |