P276-00: antineoplastic, cyclin-dependent kinase inhibitor; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 23643976 |
| CHEMBL ID | 3969723 |
| SCHEMBL ID | 665749 |
| MeSH ID | M0510667 |
| Synonym |
|---|
| 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2r,3s)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]chromen-4-one |
| gtpl7934 |
| p-276-00 |
| SCHEMBL665749 |
| p276-00 |
| 920113-02-6 |
| riviciclib |
| (+)-trans-2-(2-chlorophenyl)-8-(2-hydroxymethyl-1-methyl-pyrrolidin-3-yl)-5,7-dihydroxy-chromen-4-one |
| (+)-trans-2-(2-chlorophenyl)-5,7-dihydroxy-8-(2-hydroxy methyl-1-methyl-pyrrolidin-3-yl)-chromen-4-one |
| QLUYMIVVAYRECT-OCCSQVGLSA-N |
| (+/-)-trans-2-(2-chloro-phenyl)-5,7-dihydroxy-8-(2-hydroxymethyl-1-methyl-pyrrolidin-3-yl)-chromen-4-one |
| (+)-trans-2-(2-chloro-phenyl)-5,7-dihydroxy-8-(2-hydroxymethyl-1-methyl-pyrrolidin-3-yl)-chromen-4-one |
| CHEMBL3969723 , |
| 647019-54-3 |
| bdbm50193086 |
| 4h-1-benzopyran-4-one, 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2r,3s)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, rel- |
| Q27088556 |
| CS-0011013 |
| HY-16559A |
| P16835 |
| 4h-1-benzopyran-4-one,2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2r,3s)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-,rel- |
| A903151 |
| 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2r,3s)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-4h-1-benzopyran-4-one |
| nsc-800813 |
| nsc800813 |
| AKOS040736676 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Of the 13 patients, 11 experienced disease progression, 1 patient was withdrawn because of an adverse event (AE), and 1 patient died." | ( A phase II, single-arm, open-label, multicenter study to evaluate the efficacy and safety of P276-00, a cyclin-dependent kinase inhibitor, in patients with relapsed or refractory mantle cell lymphoma. Advani, S; Cassaday, RD; Chawla, P; Gandhi, M; Gopal, AK; Goy, A; Nachankar, R, 2015) | 0.64 |
P276-00 in combination with gemcitabine is much more effective as an antitumor agent. PANC-1 xenograft tumor model in SCID mice.
| Excerpt | Reference | Relevance |
|---|---|---|
| " We also show here that gemcitabine in combination with P276-00 is much more effective as an antitumor agent compared with either agent alone in the PANC-1 xenograft tumor model in SCID mice." | ( Molecular evidence for increased antitumor activity of gemcitabine in combination with a cyclin-dependent kinase inhibitor, P276-00 in pancreatic cancers. Joshi, K; Joshi, KS; Khanwalkar, H; Manohar, SM; Rathos, MJ, 2012) | 0.83 |
| " Phase IIb clinical trials of P276-00 in combination with gemcitabine in pancreatic cancer patients are ongoing." | ( Molecular evidence for increased antitumor activity of gemcitabine in combination with a cyclin-dependent kinase inhibitor, P276-00 in pancreatic cancers. Joshi, K; Joshi, KS; Khanwalkar, H; Manohar, SM; Rathos, MJ, 2012) | 0.87 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cyclin-T1 | Homo sapiens (human) | IC50 (µMol) | 0.0200 | 0.0010 | 0.5585 | 8.0000 | AID1317322; AID1479515; AID1572672 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 0.0790 | 0.0004 | 1.3452 | 10.0000 | AID1317305 |
| Cyclin-dependent kinase 4 | Homo sapiens (human) | IC50 (µMol) | 0.0630 | 0.0006 | 0.5706 | 10.0000 | AID1317324; AID1479514; AID1572670 |
| G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | IC50 (µMol) | 0.0790 | 0.0013 | 1.4518 | 10.0000 | AID1317305 |
| Cyclin-A2 | Homo sapiens (human) | IC50 (µMol) | 0.2240 | 0.0004 | 1.0339 | 10.0000 | AID1317321 |
| G1/S-specific cyclin-D1 | Homo sapiens (human) | IC50 (µMol) | 0.0630 | 0.0006 | 0.5479 | 9.5000 | AID1317324; AID1479514; AID1572670 |
| G1/S-specific cyclin-E1 | Homo sapiens (human) | IC50 (µMol) | 2.6700 | 0.0010 | 1.0404 | 10.0000 | AID1317323; AID1572671 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 1.8547 | 0.0004 | 1.0444 | 10.0000 | AID1317321; AID1317323; AID1572671 |
| Cyclin-dependent kinase 7 | Homo sapiens (human) | IC50 (µMol) | 2.8700 | 0.0001 | 0.9106 | 9.2000 | AID1317384 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 (µMol) | 0.0200 | 0.0010 | 0.6236 | 8.0000 | AID1317322; AID1479515; AID1572672 |
| Cyclin-H | Homo sapiens (human) | IC50 (µMol) | 2.8700 | 0.0005 | 1.0823 | 9.2000 | AID1317384 |
| CDK-activating kinase assembly factor MAT1 | Homo sapiens (human) | IC50 (µMol) | 2.8700 | 0.0030 | 1.6892 | 9.2000 | AID1317384 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1345601 | Human cyclin dependent kinase 4 (CDK4 subfamily) | 2007 | Molecular cancer therapeutics, Mar, Volume: 6, Issue:3 | In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00. |
| AID1345684 | Human cyclin dependent kinase 9 (CDK9 subfamily) | 2007 | Molecular cancer therapeutics, Mar, Volume: 6, Issue:3 | In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00. |
| AID1572670 | Inhibition of human CDK4/cyclin D1 expressed in baculovirus expression system after 30 mins in presence of [gamma-33P]ATP by scintillation counting analysis | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. |
| AID1317384 | Inhibition of CDK7/cyclin H/MAT1 (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
| AID1572673 | Antiproliferative activity against human HT-29 cells assessed as reduction in [3H]-thymidine incorporation after 48 hrs by liquid scintillation assay | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. |
| AID1479514 | Inhibition of human GST-tagged CDK4/cyclin D1 expressed in baculovirus infected insect Sf9 cells after 30 mins in presence of [32P]-gamma-ATP by scintillation counting method | |||
| AID1317321 | Inhibition of recombinant human N-terminal GST-tagged CDK2/cyclin A expressed in baculovirus expression system using retinoblastoma (792 to 928 residues) as substrate after 30 mins by gamma32P-ATP based scintillation counting analysis | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
| AID1317383 | Inhibition of CDK6/cyclin D (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
| AID1317322 | Inhibition of human CDK9 (1 to 372 residues)/cyclin T1 (1 to 726 residues) in presence of 33P-ATP by scintillation counting analysis | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
| AID1572672 | Inhibition of CDK9/cyclin T1 (unknown origin) after 30 mins in presence of [gamma-33P]ATP by scintillation counting analysis | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. |
| AID1317323 | Inhibition of human CDK2/cyclin E expressed in baculovirus infected Sf9 insect cells using retinoblastoma (792 to 928 residues) as substrate after 30 mins by gamma32P-ATP based scintillation counting analysis | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
| AID1317324 | Inhibition of human N-terminal GST-tagged CDK4/cyclin D1 expressed in baculovirus infected Sf9 insect cells using retinoblastoma (792 to 928 residues) as substrate after 30 mins by gamma32P-ATP based scintillation counting analysis | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
| AID1317305 | Inhibition of CDK1/cyclin B (unknown origin) | 2016 | Journal of medicinal chemistry, 10-13, Volume: 59, Issue:19 | Cyclin Dependent Kinase 9 Inhibitors for Cancer Therapy. |
| AID1479515 | Inhibition of full length recombinant C-terminal 6His-tagged human Cdk9/full-length human Cyclin T1 after 60 mins in presence of [33P]-gamma-ATP by filter binding assay | |||
| AID1572671 | Inhibition of human CDK2/cyclin E expressed in baculovirus expression system after 30 mins in presence of [gamma-33P]ATP by scintillation counting analysis | 2019 | Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5 | A review on flavones targeting serine/threonine protein kinases for potential anticancer drugs. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 3 (18.75) | 29.6817 |
| 2010's | 11 (68.75) | 24.3611 |
| 2020's | 2 (12.50) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (19.79) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (6.25%) | 5.53% |
| Reviews | 1 (6.25%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 14 (87.50%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||