AMG176
AMG176 Basic information
- Product Name:
- AMG176
- Synonyms:
-
- AMG176
- CS-2836
- Spiro[5,7-etheno-1H,11H-cyclobut[i][1,4]oxazepino[3,4-f][1,2,7]thiadiazacyclohexadecine-2(3H),1'(2'H)-naphthalen]-8(9H)-one, 6'-chloro-3',4',12,13,16,16a,17,18,18a,19-decahydro-16-methoxy-11,12-dimethyl-, 10,10-dioxide, (1'S,11R,12S,14E,16S,16aR,18aR)-
- Tapotoclax
- Tapotoclax（ AMG-176）
- AMG-176 (TAPOTOCLAX)
- (1S,11'R,12'S,16'S,16a'R,18a'R,E)-6-Chloro-16'-methoxy-11',12'-dimethyl-3,4,12',13',16',16a',17',18',18a',19'-decahydro-1'H,2H,3'H,11'H-spiro[naphthalene-1,2'-[5,7]ethenocyclobuta[i][1,4]oxazepino[3,4-f][1]thia[2,7]diazacyclohexadecin]-8'(9'H)-one 10',10'-dioxide
- CAS:
- 1883727-34-1
- MF:
- C33H41ClN2O5S
- MW:
- 613.21
- Mol File:
- 1883727-34-1.mol
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AMG176 Chemical Properties
- Density
- 1.32±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- 4.05±0.70(Predicted)
- color
- White to off-white
- InChIKey
- JQNINBDKGLWYMU-GEAQBIRJSA-N
- SMILES
- S1(=O)(=O)[C@H](C)[C@@H](C)CC=C[C@H](OC)[C@]2([H])CC[C@@]2([H])CN2C[C@]3(C4=C(C=C(Cl)C=C4)CCC3)COC3C=CC(=CC2=3)C(=O)N1 |t:8|
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AMG176 Usage And Synthesis
Uses
Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a Ki of 0.13 nM[1][2].
IC 50
Mcl-1: 0.13 nM (Ki)
References
[1] Caenepeel S, et al. AMG 176, a Selective MCL1 Inhibitor, is Effective in Hematological Cancer Models Alone and in Combination with Established Therapies. Cancer Discov. 2018 Sep 25. pii: CD-18-0387. DOI:10.1158/2159-8290.CD-18-0387
[2] Garner TP, et al. Progress in targeting the BCL-2 family of proteins. Curr Opin Chem Biol. 2017 Aug;39:133-142. DOI:10.1016/j.cbpa.2017.06.014
AMG176Supplier
ShangHai ChuanQian Chemcial Technique Centre Gold
- Tel
- 15869524721
- 3525679403@qq.com
ShangHai Caerulum Pharma Discovery Co., Ltd.
- Tel
- 18149758185
- sales-cpd@caerulumpharma.com
Shanghai Lollane Biological Technology Co.,Ltd.
- Tel
- 021-52996696，15000506266 15000506266
JW & Y Pharmlab Co., Ltd.
- Tel
- 021-64340559 13651849907;
- xinyu_shi@jwypharmlab.com.cn
Shanghai EFE Biological Technology Co., Ltd.
- Tel
- 021-65675885 18964387627
- info@efebio.com