This product is for research use only, not for human use. We do not sell to patients.
Size | Price | Stock |
---|---|---|
100mg | $1250 | To Be Confirmed |
200mg | $1875 | To Be Confirmed |
500mg | $3160 | To Be Confirmed |
Cat #: V40191 CAS #: 2225938-17-8 Purity ≥ 99%
Description: MS1943 (MS-1943) is a novel and potent EZH2 degrader (IC50 = 120 nM) with anticancer activity.
References: Ma A, et al. Discovery of a first-in-class EZH2 selective degrader.Nat Chem Biol. 2020 Feb;16(2):214-222.
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Molecular Weight (MW) | 718.93 |
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Molecular Formula | C42H54N8O3 |
CAS No. | 2225938-17-8 |
SMILES Code | CC(C)N(N=C1)C2=C1C(C(NCC3=C(C)C=C(C)NC3=O)=O)=CC(C4=CC=C(N=C4)N(CC5)CCN5CCNC(CC67C[C@H]8C[C@H](C[C@H](C8)C7)C6)=O)=C2 |
Synonyms | MS1943; MS 1943; MS-1943 |
Protocol | In Vitro | MS1943 (1.25-5.0 μM; 2 days) inhibits EZH2 and SUZ12 protein levels in a concentration- and timedependent manner, without affecting EED protein levels, whereas the H3K27me3 mark was also suppressed. MS1943 (0.625-5 μM; 4 days) induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells. MS1943 (0.625-5 μM; 3 days) inhibits cell growth with an GI50 of 2.2 µM. |
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In Vivo | MS1943 induces apoptosis in the MDA-MB-468 xenograft model. A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 µM and resulted in plasma concentrations above its cellular IC50 value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 µM, but plasma concentrations were below the cellular IC50 value. MS1943 (150 mg/kg body weight; i.p.; once daily for 36 days) suppresses tumor growth. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.3910 mL | 6.9548 mL | 13.9096 mL | 27.8191 mL |
5mM | 0.2782 mL | 1.3910 mL | 2.7819 mL | 5.5638 mL |
10mM | 0.1391 mL | 0.6955 mL | 1.3910 mL | 2.7819 mL |
20mM | 0.0695 mL | 0.3477 mL | 0.6955 mL | 1.3910 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.