PHA-848125

Product Name: 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);Milciclib, 10 mM in DMSO;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
CBNumber: CB92500952
Molecular Formula: C25H32N8O
Formula Weight: 460.57
MOL File: 802539-81-7.mol

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PHA-848125 Property

Melting point:: 190 °C
Density: 1.33
storage temp.: Store at -20°C
solubility: ≥23.05 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
form: solid
pka: 14.44±0.40(Predicted)
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 21474
Product name: PHA-848125
Purity: ≥98%
Packaging: 1mg
Price: $62
Updated: 2024/03/01

Cayman Chemical

Product number: 21474
Product name: PHA-848125
Purity: ≥98%
Packaging: 5mg
Price: $135
Updated: 2024/03/01

Cayman Chemical

Product number: 21474
Product name: PHA-848125
Packaging: 10mg
Price: $239
Updated: 2024/03/01

TRC

Product number: P294490
Product name: PHA-848125
Packaging: 2.5mg
Price: $130
Updated: 2021/12/16

Usbiological

Product number: 462344
Product name: PHA-848125
Packaging: 2.5mg
Price: $425
Updated: 2021/12/16

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PHA-848125 Chemical Properties,Usage,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)

target

CDK2/CyclinA

References

1. brasca mg, amboldi n, ballinari d et al. identification of n,1,4,4-tetramethyl-8-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-4,5-dihydro-1h-pyrazolo[4,3-h]quinazoline-3-carboxamide (pha-848125), a potent, orally available cyclin dependent kinase inhibitor. j med chem. 2009 aug 27;52(16):5152-63.

PHA-848125 Preparation Products And Raw materials

Raw materials

Preparation Products

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PHA-848125 Suppliers

China 83 India 2 United States 16 Global 101

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802539-81-7, PHA-848125Related Search:

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PHA-848125

4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide

Milciclib

PHA-848125 (Milciclib)

Milciclib (PHA-848125)

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 PHA 848125

4,5-Dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-1H-pyrazolo[4,3-h]

PHA-84812

1H-Pyrazolo[4,3-h]quinazoline-3-carboxamide, 4,5-dihydro-N,1,4,4-tetramethyl-8-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-

PHA-848125 USP/EP/BP

Milciclib, 10 mM in DMSO

802539-81-7

Inhibitors