Basic information Safety Supplier Related

MK-8998

Basic information Safety Supplier Related

MK-8998 Basic information

Product Name:
MK-8998
Synonyms:
  • MK-8998
  • (R)-2-(4-isopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetaMide
  • MK8998;MK 8998
  • CS-2435
  • CX-8998
  • Benzeneacetamide, 4-(1-methylethyl)-N-[(1R)-1-[5-(2,2,2-trifluoroethoxy)-2-pyridinyl]ethyl]-
  • Suvecaltamide
  • inhibit,MK 8998,Calcium Channel,Ca channels,Inhibitor,Suvecaltamide,Ca2+ channels,MK8998
CAS:
953778-58-0
MF:
C20H23F3N2O2
MW:
380.4
Product Categories:
  • API
Mol File:
953778-58-0.mol
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MK-8998 Chemical Properties

Boiling point:
510.3±50.0 °C(Predicted)
Density 
1.178±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : ≥ 100 mg/mL (262.88 mM);Water : < 0.1 mg/mL (insoluble)
pka
14.27±0.46(Predicted)
form 
Solid
color 
White to off-white
InChI
InChI=1S/C20H23F3N2O2/c1-13(2)16-6-4-15(5-7-16)10-19(26)25-14(3)18-9-8-17(11-24-18)27-12-20(21,22)23/h4-9,11,13-14H,10,12H2,1-3H3,(H,25,26)/t14-/m1/s1
InChIKey
IQIKXZMPPBEWAD-CQSZACIVSA-N
SMILES
C1(CC(N[C@@H](C2=NC=C(OCC(F)(F)F)C=C2)C)=O)=CC=C(C(C)C)C=C1
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MK-8998 Usage And Synthesis

Uses

Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth[1].

in vivo

Suvecaltamide (3-30 mg/kg, once daily for 28 days, orally) reverses the peripheral nerve toxicity (CIPN) induced by Bortezomib (BTZ, HY-10227) in a rat model[1].
Suvecaltamide (30 mg/kg, once daily for 28 days, orally) reduces tumor volume in a xenograft mouse model of human multiple myeloma without affecting the anti-cancer activity of BTZ[1].

Animal Model:BTZ-Induced CIPN Rat Model[1]
Dosage:3, 10, 30 mg/kg; once daily for 28 days
Administration:orally
Result:Increased raised the nerve conduction velocity (NCV) levels of the tail nerve and sciatic nerve by dose-dependent.
Reduced the β-tubulin polymerization caused by BTZ and increased the number of cutaneous unmyelinated fiber in the hindpaw (IENF) at 30 mg/kg, without affecting proteasome activity.
Animal Model:a START cell-based xenograft athymic nude mouse tumor model of human myeloma[1]
Dosage:30 mg/kg, once daily for 28 days
Administration:orally
Result:Reduced the size of the tumor without affecting the anti-cancer activity of BTZ or the weight loss effects.

IC 50

T-type calcium channel

References

[1] Cristina Meregalli, et al. Reversal of Bortezomib-Induced Neurotoxicity by Suvecaltamide, a Selective T-Type Ca-Channel Modulator, in Preclinical Models. Cancers (Basel). 2021 Oct 7;13(19):5013. DOI:10.3390/cancers13195013

MK-8998Supplier

MQ (shanghai) Pharmaceuticals Co., Ltd. Gold
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13761635123
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Shanghai Boyle Chemical Co., Ltd.
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Shanghai Hope Chem Co., Ltd.，
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+21-18501659228 18501659228
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ShangHai Onsyn-Chemical Technology Co., Ltd.
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shanghai cooperpharm co.,LTD .
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+86-021-58975553
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sales@cooperpharm.com
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MK-8998(953778-58-0)Related Product Information