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920113-03-7 (P276-00)

1

Identification

P276-00 P276-00
Name P276-00
Formula C21H21Cl2NO5
MW 438.3
CAS No. 920113-03-7
EINECS
Smiles [H]Cl.O=C1C=C(C2=CC=CC=C2Cl)OC3=C([[email protected]@H]4CCN(C)[[email protected]]4CO)C(O)=CC(O)=C31
Synonyms P276; 2-(2-chlorophenyl)-5,7-dihydroxy-8-((2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4H-chromen-4-one hydrochloride
InChI InChI=1S/C21H20ClNO5.ClH/c1-23-7-6-12(14(23)10-24)19-15(25)8-16(26)20-17(27)9-18(28-21(19)20)11-4-2-3-5-13(11)22;/h2-5,8-9,12,14,24-26H,6-7,10H2,1H3;1H/t12-,14+;/m1./s1
2

Introduction

P276-00 is a flavone and cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity.

Background Information

p276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. P276-00 induces apoptosis in multiple myeloma cells by inhibition of Cdk9-T1 and RNA polymerase II-dependent transcription. P276-00 showed a potent cytotoxic effect against MCL cell lines. P276-00 causes multiple myeloma cell death by disrupting the balance between cell survival and apoptosis through inhibition of transcription and downregulation of Mcl-1. P276-00 alone or in combination is a potential therapeutic molecule to improve patients' outcome in mantle cell lymphoma. P276-00 induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models. ......by AbMole BioScience
P276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. In Phase 2/3 ......by AdooQ BioScience, LLC
P276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. ......by BOC Sciences
Riviciclib, also known as P276-00 , is a flavone and cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. P276-00 selectively binds to and inhibits Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, serine/threonine kinases that play key roles in the regulation of the cell cycle and cellular proliferation. Inhibition of these kinases leads to cell cycle arrest during the G1/S transition, thereby leading to an induction of apoptosis, and inhibition of tumor cell proliferation. ......by MedKoo Biosciences, Inc.
A novel potent CDK inhibitor with IC50 of 79 nM, 63 nM and 20 nM for Cdk4/cyclin D1, Cdk1/cyclin B and Cdk9/cyclin T1, respectively; weakly inhibits Cdk2/cyclin A, Cdk2/cyclin E, Cdk6/cyclin D3 and Cdk7/cyclin H with IC50 of 0.2-3 uM; shows potent antiproliferative effects against various human cancer cell lines (IC50=200-800 nM); induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models.Pancreatic CancerPhase 2 Clinical ......by ProbeChem
P276-00 is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. Phase 2/3. ......by Selleck Chemicals LLC
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance: EBNumber:EB000018110

Storage condition

Solubility

DMSO 88 mg/mL (200 mM) ; Water 88 mg/mL (200 mM) ; Ethanol 7 mg/mL (15 mM) by Selleck Chemicals LLC
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Mechanism and Indication

Signaling Pathways Cell Cycle/DNA Damage
Target CDK
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
P276-00 - No Development Reported
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Safety Data of P276-00

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AbMole BioScience USA
AdooQ BioScience, LLC USA
Ark Pharm, Inc. USA
BOC Sciences
Biochempartner Co., Ltd China
MedKoo Biosciences, Inc. USA
ProbeChem
Selleck Chemicals LLC 5mg/USD270(In stock);50mg/USD1070(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
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Related Products

Other Forms of 920113-03-7

Name CAS No Formula MW
P276-00 (free base) 920113-02-6 C21H20ClNO5 401.84

Recommended Compounds in CDK

Name CAS No Formula MW
LY2857785 1619903-54-6 C26H36N6O 448.6
THZ2 1604810-84-5 C31H28ClN7O2 566.0527
Palbociclib (isethionate) 827022-33-3 C26H35N7O6S 573.66
CDK9-IN-6 1391855-95-0 C27H37ClN6O2 513.07468
ML167 1285702-20-6 C19H17N3O3 335.36
AMG 925 1401033-86-0 C26H29N7O2 471.55
LDC000067 1073485-20-7 C18H18N4O3S 370.43
LEE011 (succinate hydrate) 1374639-79-8 C27H38N8O6X 570.64
LEE011 (succinate) 1374639-75-4 C27H36N8O5 552.63
LEE011 (hydrochloride) 1211443-80-9 C23H31ClN8O 471.0
LEE011 1211441-98-3 C23H30N8O 434.54
WHI-P180 (hydrochloride) 153437-55-9 C16H16ClN3O3 333.77
Wogonin 632-85-9 C16H12O5 284.26
1-NM-PP1 221244-14-0 C20H21N5 331.41
WHI-P180 211555-08-7 C16H15N3O3 297.31
THZ1 1604810-83-4 C31H28ClN7O2 566.05
Senexin A 1366002-50-7 C17H14N4 274.32
CDK4-IN-1 1256963-02-6 C22H29ClN8 440.97
Palbociclib (hydrochloride) 827022-32-2 C24H30ClN7O2 483.99
Purvalanol B 212844-54-7 C20H25ClN6O3 432.9

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

Protocol Reference

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More Information

P276-00

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