Successful, we will reply to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
Products are for research use only. Not for human use. We do not sell to patients.
(L868275; HMR-1275; Alvocidib)
Flavopiridol Chemical Structure
|Product name: Flavopiridol|
|Cat. No.: HY-10005|
Flavopiridol competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initially found to inhibit EGFR and PKA.
IC50 Value: ~ 40 nM
in vitro: Flavopiridol induces G1 arrest with inhibition of CDK2 and CDK4 in human breast carcinoma cells in a time and concentration dependent manner. Short time treatment of Flavopiridol (~12 hours) induce apoptosis in hematopoietic cell lines including SUDHL4, SUDHL6 (B-cell lines), Jurkat and MOLT4 (T-cell lines ), and HL60 (myeloid). In the clonogenic assay, Flavopiridol functions as a highly potent cytotoxic compound with a mean IC70 with 8 ng/mL in 23 human tumor models. A recent study shows Flavopiridol treatment induces a substantial AKT-Ser473 phosphorylation in human glioblastoma T98G cell line.
in vivo: After treatment with 7.5 mg/kg Flavopiridol bolus intravenous (IV) or intraperitoneal on each of 5 consecutive days, 11 out of 12 advanced stage subcutaneous (s.c.) human HL-60 xenografts undergo complete regressions, and animals remain disease-free several months after one course of Flavopiridol treatment. SUDHL-4 s.c. lymphomas treated with flavopiridol at 7.5 mg/kg bolus IV for 5 days undergo either major (two out of eight mice) or complete (four out of eight mice) regression, with two animals remaining disease-free for more than 60 days. The overall growth delay is 73.2%.
|M.Wt||401.84||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.4886 mL||12.4428 mL||24.8855 mL|
|5 mM||0.4977 mL||2.4886 mL||4.9771 mL|
|10 mM||0.2489 mL||1.2443 mL||2.4886 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|Flavopiridol||Testis tumor||31-MAY-13||30-SEP-13||Phase 2||06-SEP-13|
|Ovary tumor||31-MAY-13||30-SEP-13||Phase 2||06-SEP-13|
|Sidney Kimmel Comprehensive Cancer Center||Acute myelogenous leukemia||31-MAY-11||31-JUL-13||Phase 2||14-SEP-13|
|Eastern Cooperative Oncology Group||Acute myelogenous leukemia||31-OCT-08||Phase 2||05-AUG-13|
|Sidney Kimmel Comprehensive Cancer Center||Acute myelogenous leukemia||30-APR-11||Phase 2||17-JUL-13|
. Mahoney E, Lucas DM, Gupta SV, Wagner AJ, Herman SE, Smith LL, Yeh YY, Andritsos L, Jones JA, Flynn JM, Blum KA, Zhang X, Lehman A, Kong H, Gurcan M, Grever MR, Johnson AJ, Byrd JC.ER stress and autophagy: new discoveries in the mechanism of action and drug resistance of the cyclin-dependent kinase inhibitor flavopiridol.Blood. 2012 Aug 9;120(6):1262-73. Epub 2012 Jun 27.
. Karp JE, Garrett-Mayer EL, Estey EH, Rudek MA, Smith BD, Greer JM, Drye DM, Mackey K, Dorcy KS, Gore SD, Levis MJ, McDevitt MA, Carraway HE, Pratz KW, Gladstone DE, Showell MM, Othus M, Doyle LA, Wright JJ, Pagel JM.Randomized phase II study of two schedules of flavopiridol given as timed sequential therapy with cytosine arabinoside and mitoxantrone for adults with newly diagnosed, poor-risk acute myelogenous leukemia.Haematologica. 2012 Jun 24.
. Bible KC, Peethambaram PP, Oberg AL, Maples W, Groteluschen DL, Boente M, Burton JK, Gomez Dahl LC, Tibodeau JD, Isham CR, Maguire JL, Shridhar V, Kukla AK, Voll KJ, Mauer MJ, Colevas AD, Wright J, Doyle LA, Erlichman C; the Mayo Phase 2 Consortium (P2C) and North Central Cancer Treatment Group (NCCTG).A Phase 2 Trial of Flavopiridol (Alvocidib) and Cisplatin in Platin-Resistant Ovarian and Primary Peritoneal Carcinoma: MC0261.Gynecol Oncol. 2012 Oct;127(1):55-62. Epub 2012 Jun 1.
CAS No.: 131740-09-5 In-stock
1NM-PP1(PP1 Analog II) is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors(IC50=28 uM vSrc; 4.2 nM v-Src-as1 I338G).
AMG 925 is a potent and selective dual inhibtor of CDK4/FLT3 with IC50s of 1.5 nM and 2.4 nM for CDK4 and FLT3, respectively; with IC50 of 19 nM in MOLM-13 cell.
AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM. It is less potent to CDK5/6.
6-BIO(6-Bromoindirubin-3(acute)-oxime) is a potent and selective inhibitor of GSK-3 and CDK1–cyclinB complex with IC50 of 5 nM /320 nM/83 nM for GSK-3(alpha)(beta)/CDK1/CDK5 respectively.
BMS-265246 is a potent and selective CDK1/2 inhibitor for CDK1/cyclin B and CDK2/cyclin E with IC50 of 6 nM and 9 nM, respectively.
Briciclib is a small molecule that suppresses cyclin D1 accumulation in cancer cells.
Ca2(addition) channel agonist 1 is a N-type Ca2(addition) channel activity agonist, with EC50 of 14.23 uM, also inhibits cdk2 kinase activity with EC50 of 3.34 uM.
CDK-IN-2 is a potent and specific CDK9 inhibitor with IC50 of <8 nM.
CDK9-IN-1 is a novel, selective CDK9 inhibitor for the treatment of HIV infection.
CDK9-IN-2 is a novel cyclin-dependent kinase 9(CDK9) inhibitor.