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S-63845
CAS No. 1799633-27-4
S-63845( S 63845 | S63845 )
Catalog No. M12723 CAS No. 1799633-27-4
S-63845 (S63845) is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 133 | In Stock |
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| 10MG | 222 | In Stock |
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| 25MG | 399 | In Stock |
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| 100MG | Get Quote | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameS-63845
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NoteResearch use only, not for human use.
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Brief DescriptionS-63845 (S63845) is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM.
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DescriptionS-63845 (S63845) is a highly potent, selective Mcl-1 inhibitor with Kd of 0.19 nM, with no appreciable binding affinity to BCL-2 or BCL-XL (Ki>10 uM); binds to the BH3-binding groove of Mcl-1, potently kills MCL1-dependent cancer cells, including multiple myeloma (IC50<0.1 uM), leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway; is well tolerated and shopws high effectivity against mouse cancer models.Blood Cancer Preclinical.
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In VitroThe pro-survival protein myeloid cell leukemia 1 (MCL1) is over expressed in many cancers. S63845 is a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. The activity of S63845 is next evaluated in a panel of eight AML cell lines: all lines are sensitive to S63845 (IC50=4-233 nM).
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In VivoS63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice, with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg, S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model.
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SynonymsS 63845 | S63845
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PathwayAngiogenesis
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TargetBcl-2
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RecptorBcl-2
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number1799633-27-4
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Formula Weight829.2593
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Molecular FormulaC39H37ClF4N6O6S
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Purity>98% (HPLC)
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SolubilityDMSO
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SMILESO=C(O)[C@@H](CC1=C(OCC2=CC=NN2CC(F)(F)F)C=CC=C1)OC3=C4C(SC(C5=CC=C(F)O5)=[C@@]4[C@@]6=C(C)C(Cl)=C(OCCN7CCN(C)CC7)C=C6)=NC=N3
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Chemical NameDispiro[cyclohexane-1,2'-[2H]indene-1'(3'H),2''-[2H]imidazol]-4''-amine, 4-methoxy-5''-methyl-6'-[5-(1-propyn-1-yl)-3-pyridinyl]-, (1α,1'R,4β)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Kotschy A, et al. Nature. 2016 Oct 27;538(7626):477-482.
2. Merino D, et al. Sci Transl Med. 2017 Aug 2;9(401). pii: eaam7049.
3. Letai A. Cancer Cell. 2016 Dec 12;30(6):834-835.
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