CFI-400945
- Product Name
- CFI-400945
- CAS No.
- 1338806-73-7
- Chemical Name
- CFI-400945
- Synonyms
- CFI-400945;ocifisertib;CFI-400945 (CFI400945;CFI-400945 (free base);Ocifisertib（CFI-400945 free base）;CFI400945 free base,CFI 400945 free base;Ocifisertib（CFI-400945 free base）, 10 mM in DMSO;(1R,2S)-2-(3-((E)-4-(((2R,6S)-2,6-Dimethylmorpholino)methyl)styryl)-1H-indazol-6-yl)-5'-methoxyspiro[cyclopropane-1,3'-indolin]-2'-one;(1R,2S)-2-[3-[(E)-2-[4-[[(2S,6R)-2,6-dimethylmorpholin-4-yl]methyl]phenyl]vinyl]-1H-indazol-6-yl]-5'-methoxy-spiro[cyclopropane-1,3'-indoline]-2'-one;Spiro[cyclopropane-1,3'-[3H]indol]-2'(1'H)-one, 2-[3-[(1E)-2-[4-[[(2R,6S)-2,6-dimethyl-4-morpholinyl]methyl]phenyl]ethenyl]-1H-indazol-6-yl]-5'-methoxy-, (1R,2S)-
- CBNumber
- CB92716177
- Molecular Formula
- C33H34N4O3
- Formula Weight
- 534.65
- MOL File
- 1338806-73-7.mol
CFI-400945 Property
- Boiling point:
- 751.5±60.0 °C(Predicted)
- Density
- 1.32±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- insoluble in H2O; ≥109.8 mg/mL in DMSO; ≥93 mg/mL in EtOH
- form
- crystalline solid
- pka
- 13.09±0.40(Predicted)
- color
- White to yellow
N-Bromosuccinimide Price
- Product number
- C5813
- Product name
- CFI-400945
- Packaging
- 5mg
- Price
- $154
- Updated
- 2021/12/16
- Product number
- C5813
- Product name
- CFI-400945
- Packaging
- 10mM(in 1mL DMSO)
- Price
- $182
- Updated
- 2021/12/16
- Product number
- C5813
- Product name
- CFI-400945
- Packaging
- 10mg
- Price
- $257
- Updated
- 2021/12/16
- Product number
- orb611612
- Product name
- CFI-400945
- Packaging
- 100mg
- Price
- $765
- Updated
- 2021/12/16
- Product number
- C5813
- Product name
- CFI-400945
- Packaging
- 50mg
- Price
- $926
- Updated
- 2021/12/16
CFI-400945 Chemical Properties,Usage,Production
Uses
(1R,?2S)?-2-?[3-?[(1E)?-?2-?[4-?[[(2R,?6S)?-?2,?6-?Dimethyl-?4-?morpholinyl]?methyl]?phenyl]?ethenyl]?-?1H-?indazol-?6-?yl]?-?5''-?methoxy-?spiro[cyclopropane-?1,?3''-?[3H]?indol]?-?2''(1''H)?-?one selectively inhibits polo-like kinase 4 (PLK4), which is a serine/threonine protein kinase that regulates centriole duplication during the cell cycle. PLK4 is a therapeutic target for various cancers.
Biological Activity
cfi-400945 is an orally active, potent and selective inhibitor of polo-like kinase 4.polo-like kinase 4 (plk4), a unique member of the polo-like family of kinases, shares little homology with other polo-like kinases. plk4 plays an essential role in centriole duplication. overexpression of plk4 overrides the centriole licensing mechanism and results in centriole amplification with multiple procentrioles forming around each parental centriole. depletion of plk4 by rnai prevents the formation of abnormal centrioles and microtubule-based structures, causing mitotic defects and in some cell lines it can induce apoptosis [2].in an assay using recombinant human plk4, cfi-400945 inhibited plk4 with an ic50 value of 2.8 ± 1.4 nm in an atp competitive manner with a ki value of 0.26 ± 0.1 nm. cfi-400945 inhibited autophosphorylation of plk4 at serine 305 with an ec50 value of 12.3 nm in cells overexpressing plk4 [1]. cfi-400945 showed no significant inhibitory activity against other plk family members (plk1, plk2, and plk3 with the ic50s of > 50 μm. in transfected hct116 cells with trka, trkb, and tie2/tek, the ec50 values were 84 nm, 88 nm, and 117 nm, respectively. cfi-400945 inhibited the activity of aurka and aurkb with the ec50 value of 510 nm and 102 nm. cfi-400945 (≥ 200 nm) decreased the mean centriole number in asynchronous u2os cells [1]. cfi-400945 inhibited a panel of breast cancer cell growth with the gi50 of 14-165 nm. in mice, the maximum tolerated dose (mtd) of cfi-400945 for once-daily oral administration was estimated to be 7.5-9.5 mg/kg [1].
References
[1] mason j m, lin d c c, wei x, et al. functional characterization of cfi-400945, a polo-like kinase 4 inhibitor, as a potential anticancer agent[j]. cancer cell, 2014, 26(2): 163-176.
[2] sillibourne j e, bornens m. polo-like kinase 4: the odd one out of the family[j]. cell division, 2010, 5(1): 25.
CFI-400945 Preparation Products And Raw materials
Raw materials
Preparation Products
CFI-400945 Suppliers
- Tel
- Fax
- 86-21-57758967
- sales@boylechem.com
- Country
- China
- ProdList
- 2922
- Advantage
- 55
- Tel
- 0-1502103-5486 18017383231
- Fax
- qq：2817624287
- 983544897@qq.com
- Country
- China
- ProdList
- 9347
- Advantage
- 55
- Tel
- 18149758185 18149758185
- sales-cpd@caerulumpharma.com
- Country
- China
- ProdList
- 3466
- Advantage
- 58
- Tel
- 15901859516
- Fax
- 15901859516
- sales@DKMbiochem.com
- Country
- China
- ProdList
- 344
- Advantage
- 58
- Tel
- 021-24206007 13764915196
- Fax
- 86-021-23027023
- sales@balmxy.com
- Country
- China
- ProdList
- 6790
- Advantage
- 55
- Tel
- 021-52996696，15000506266 15000506266
- Fax
- +86-21-52996696
- Country
- China
- ProdList
- 4599
- Advantage
- 55
- Tel
- Fax
- -
- eric_feng1954@126.com
- Country
- China
- ProdList
- 9248
- Advantage
- 55
- Tel
- 021-65675885 18964387627
- Fax
- 021-65675885
- info@efebio.com
- Country
- China
- ProdList
- 9804
- Advantage
- 58
- Tel
- 17754423994 17754423994
- Fax
- QQ:2853530913
- 2853530910@QQ.com
- Country
- China
- ProdList
- 8010
- Advantage
- 62
- Tel
- 21-31433387 15618786686
- Fax
- QQ:1369748377
- sales@rechemscience.com
- Country
- China
- ProdList
- 2986
- Advantage
- 58
- Tel
- 021-QQ：65489617 15618227136
- Fax
- 21-5161 9052
- Sales@ATKchemical.com
- Country
- China
- ProdList
- 9014
- Advantage
- 58
- Tel
- 010-50973130 4009686088
- 3193328036@qq.com
- Country
- China
- ProdList
- 29764
- Advantage
- 68
- Tel
- 571-89925085
- Fax
- 0086-571-89925065
- sales@amadischem.com
- Country
- China
- ProdList
- 131957
- Advantage
- 58
- Tel
- +86-13168912896
- Country
- China
- ProdList
- 253
- Advantage
- 58
- Tel
- 0550-5196001 15000891977
- Fax
- 0550-5196001
- wj520wjxby@126.com
- Country
- China
- ProdList
- 1927
- Advantage
- 55
- Tel
- +86 18721201413
- Fax
- +86 (21) 5775-8967
- sales@biopharmaleader.com
- Country
- China
- ProdList
- 1720
- Advantage
- 58
- Tel
- 021-58111628 15800915896
- Fax
- QQ 3285589261
- sales@twochem.com
- Country
- China
- ProdList
- 1788
- Advantage
- 58
- Tel
- 020-31155029 18902330969
- Fax
- 020-31155029
- sales@tomums.cn
- Country
- China
- ProdList
- 4696
- Advantage
- 58
- Tel
- 18081075745
- chemflowtech@sina.com
- Country
- China
- ProdList
- 1886
- Advantage
- 58
- Tel
- 0371-0371-55055611 18137792234
- Fax
- QQ：3002694073
- 3002694073@qq.com
- Country
- China
- ProdList
- 10532
- Advantage
- 58
- Tel
- Country
- China
- ProdList
- 13179
- Advantage
- 58
- Tel
- +1-2135480471 +1-2135480471
- sales@sarms4muscle.com
- Country
- China
- ProdList
- 10473
- Advantage
- 58
- Tel
- 13969155946
- 1461866103@qq.com
- Country
- China
- ProdList
- 16111
- Advantage
- 58
- Tel
- 63313187 15358055255
- Fax
- QQ：63313187
- 63313187@qq.com
- Country
- China
- ProdList
- 1990
- Advantage
- 58
- Tel
- 18818260767
- Fax
- QQ 3610331285
- sales@chemegen.com
- Country
- China
- ProdList
- 11218
- Advantage
- 58
- Tel
- 021-38015121 18438616290
- wulan@absin.cn
- Country
- China
- ProdList
- 24731
- Advantage
- 58
- Tel
- 88888888888
- hongquchem@qq.com
- Country
- China
- ProdList
- 5132
- Advantage
- 58
- Tel
- 15727060112
- yutianchun2007@126.com
- Country
- China
- ProdList
- 10001
- Advantage
- 58
- Tel
- 021-58432009 400-005-6266
- Fax
- 021-58436166
- marketing1@energy-chemical.com
- Country
- China
- ProdList
- 44811
- Advantage
- 58
- Tel
- 0519-85524369
- 3477467573@qq.com
- Country
- China
- ProdList
- 8617
- Advantage
- 58
- Tel
- 15720605021
- Fax
- QQ：353175721
- zhang_lei@jsnchem.com
- Country
- China
- ProdList
- 1724
- Advantage
- 58
- Tel
- 027-59101668 19945030958
- Fax
- 027-59101668
- 2881924765@qq.com
- Country
- China
- ProdList
- 7960
- Advantage
- 58
- Tel
- 400-1647117 13681763483
- product02@bidepharm.com
- Country
- China
- ProdList
- 62072
- Advantage
- 58
- Tel
- 15870833005
- 2232044025@qq.com
- Country
- China
- ProdList
- 8206
- Advantage
- 58
- Tel
- 13549236410
- sales@invivochem.cn
- Country
- China
- ProdList
- 6753
- Advantage
- 58
- Tel
- 17771424646
- shoubull@126.com
- Country
- China
- ProdList
- 990
- Advantage
- 58
- Tel
- 18662190603
- 437347250@qq.com
- Country
- China
- ProdList
- 7325
- Advantage
- 58
- Tel
- +86-027-59232304 15387063101
- 2881924050@qq.com
- Country
- China
- ProdList
- 9998
- Advantage
- 58
- Tel
- 4008200310
- marketing@tsbiochem.com
- Country
- China
- ProdList
- 24641
- Advantage
- 58
- Tel
- 4000255188 4000255188
- sales@pharmablock.com
- Country
- China
- ProdList
- 7268
- Advantage
- 58
- Tel
- 400-6206333 1316706386
- anhua.mao@aladdin-e.com
- Country
- China
- ProdList
- 48458
- Advantage
- 58
- Tel
- 17721492509; 17721492509
- 643638326@qq.com
- Country
- China
- ProdList
- 4944
- Advantage
- 58
- Tel
- 17316404525
- 209533805@qq.com
- Country
- China
- ProdList
- 9973
- Advantage
- 58
- Tel
- 400-821-026
- Sales@sangon.com
- Country
- China
- ProdList
- 47255
- Advantage
- 58
- Tel
- 80-Enzo Biochem Inc. 18009420430
- info-usa@enzolifesciences.com
- Country
- China
- ProdList
- 124812
- Advantage
- 58
- Tel
- 18964309092 18964309092
- 2769493375@qq.com
- Country
- China
- ProdList
- 919
- Advantage
- 58
- Tel
- +undefined-21-51877795
- Fax
- +86 21 5161 9052/ 5187 7796
- ivan@atkchemical.com
- Country
- China
- ProdList
- 33024
- Advantage
- 60
- Tel
- +86-512-68323658 +86-18168183658
- sales1@artkmedchem.com
- Country
- China
- ProdList
- 39003
- Advantage
- 58
- Tel
- --
- Fax
- --
- info@neobioscience.com
- Country
- CHINA
- ProdList
- 6207
- Advantage
- 58
- Tel
- --
- Fax
- --
- chenjw@absin.cn
- Country
- CHINA
- ProdList
- 6213
- Advantage
- 58