PHA-848125
- CAS No.
- 802539-81-7
- Chemical Name:
- PHA-848125
- Synonyms
- Milciclib;PHA-84812;PHA-848125;PHA-848125 USP/EP/BP;Milciclib (PHA-848125);PHA-848125 (Milciclib);4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h];N,1,4,4-tetramethyl-8-(4-(4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide;1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-
- CBNumber:
- CB92500952
- Molecular Formula:
- C25H32N8O
- Molecular Weight:
- 460.57
- MOL File:
- 802539-81-7.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/2 8:55:41
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302 | |||||||||
| Precautionary statements | P280-P305+P351+P338 | |||||||||
| NFPA 704 |
|
PHA-848125 Chemical Properties,Uses,Production
Description
PHA-848125 is an ATP-competitive inhibitor of cyclin-dependent kinases (Cdks) that potently inhibits Cdk2/cyclin A (IC50 = 45 nM). It is at least 3-fold less potent at Cdks 1, 3, 4, 5, and 7. PHA-848125 is orally available and displays efficacy in suppressing the growth of cancer cells or tumor xenografts in animals.
Uses
PHA-848125 is a cyclin dependent kinase (CDK) inhibitor. Oral PHA-848125 showed antitumor activity via dual targeting of cyclin-dependent kinase and tropomyosin receptor kinase families in human carcinoma cell and xenografted mouse model of carcinoma.
Enzyme inhibitor
This cyclin kinase-directed inhibitor (FW = 460.57 g/mol; CAS 802539-81- 7, 802540-32-5 (3HCl), 1253645-38-3 (Maleic acid); Solubility: 90 mg/mL DMSO; <1 mg/mL Water), systematically named N,1,4,4-tetramethyl-8-(4- (4-methylpiperazin-1-yl)phenylamino)-4,5-dihydro-1H-pyrazolo[4,3-h] quinazoline-3-carboxamide, targets cyclin A/CDK2 inhibitor with IC50 of 45 nM. PHA-848125-treated cells show cell cycle arrest in G1 and reduced DNA synthesis, accompanied by inhibition of pRb phosphorylation and modulation of other CDK-dependent markers. Cyclin Target Selectivity: Cdk1 (weak, if any), Cdk2 (++), Cdk3 (weak, if any), Cdk4 (weak, if any), Cdk5 (weak, if any), Cdk6 (weak, if any), Cdk7 (weak, if any), Cdk8 (weak, if any), Cdk9 (weak, if any), Cdk10 (weak, if any)
PHA-848125 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 | China | 9337 | 55 | Inquiry |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | China | 32836 | 60 | Inquiry |
| BOC Sciences | +1-631-485-4226 | United States | 19553 | 58 | Inquiry |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | China | 49392 | 58 | Inquiry |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | China | 24200 | 58 | Inquiry |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | China | 10522 | 58 | Inquiry |
| InvivoChem | +1-708-310-1919 +1-13798911105 | United States | 6393 | 58 | Inquiry |
| TargetMol Chemicals Inc. | +1-781-999-5354 | United States | 19973 | 58 | Inquiry |