RP-6685 - ≥99% , CAS No.2832047-80-8

CAS: 2832047-80-8 Cat. No.: R647344 Summenformel: C₂₂H₁₄F₇N₅O Molekulargewicht: 497.37

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Übersicht

RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC 50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model

In Vitro

RP-6685 is extremely potent with an IC 50 of 550 pM against the pol activity of full-length Polθ and inactive on the ATPase activity. RP-6685 inhibits Polθ in HEK293 LIG4 -/- cellswith an IC 50 of 0.94 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

RP-6685 (80 mg/kg; p.o.; BID for 21 days) exhibits potent antitumor efficacy in BRCA2-deficient HCT116 mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD1 nude mice (HCT116 BRCA2 +/+ and BRCA2 -/- xenograft tumor models) Dosage: 80 mg/kg Administration: p.o.; BID for 21 days Result: Showed tumor regression during the first 8 days of treatment in BRCA2 -/- HCT116 model, while did not inhibit tumor growth in BRCA2 +/+ HCT116 tumors mice. Animal Model: CD1 mice (20-30 g) Dosage: 2.5 mg/kg Administration: i.v. or p.o.; single dosage Result: CL (mL/min/kg) V dss (L/kg) t 1/2 (h) F (%) 36.8 1.1 0.4 66

Form:Solid

IC50& Target:IC 50 : 5.8 nM (Polθ)

Specifications

Spezifikationen & Reinheit

≥99%

Biochemische und physiologische Mechanismen

RP-6685 is a potent, selective and orally active DNA polymerase theta (Polθ) inhibitor with an IC 50 value of 5.8 nM (PicoGreen assay). RP-6685 shows antitumor efficacy in mouse tumor xenograft model.

Storage

Store at -20°C

Verschickt in

Ice chest + Ice pads

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Reinheit

≥99%

Namen und Kennungen

• Kanonisches Lächeln: O=C(N(CC#CC1=NN=C(N)C=C1)C2=CC=C(F)C=C2)CC3=NC=C(C(F)(F)F)C=C3C(F)(F)F
• Molekulargewicht: 497.37

Chemische und physikalische Eigenschaften

• Löslichkeit: DMSO : 100 mg/mL (201.06 mM; Need ultrasonic)