2. MAPK/ERK Pathway
  3. MEK
  4. Tunlametinib

Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer).

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Tunlametinib Chemical Structure

Tunlametinib Chemical Structure

CAS No. : 1801756-06-8

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Based on 1 publication(s) in Google Scholar

Tunlametinib Related Antibodies

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Description

Tunlametinib is a highly selective, orally active MEK1/2 inhibitor (IC50=1.9 nM, MEK1). Tunlametinib blocks the RAS-RAF-MEK-ERK signaling pathway, arrests tumor cell cycle and promotes apoptosis. Tunlametinib potently inhibits the proliferation of RAS/RAF mutant cancer cells (such as BRAF V600E, KRAS G12C mutant cells). Tunlametinib shows synergistic anti-tumor effects with BRAF/KRASG12C/SHP2 inhibitors, Docetaxel (HY-B0011). Tunlametinib can be used to study targeted therapy for RAS/RAF mutation-driven malignancies (such as melanoma, colorectal cancer, and non-small cell lung cancer)[1][2].

IC50 & Target

MEK1

 

MEK2

 

In Vitro

Tunlametinib inhibits the cell viability of BRAF/KRAS mutant cell lines: A375, Colo-829, HL-60 melanoma cells, COLO 205, HT-29 colon cancer cells, Calu-6, A549 lung cancer cells, with IC50 of 0.86 nM, 3.46 nM, 0.67 nM, 0.94 nM, 10.07 nM, 59.89 nM, respectively. Tunlametinib has no significant effect on RAS/RAF wild-type cells (H1975, MRC-5)[1].
Tunlametinib (1-9 nM; 48 h) dose-dependently increases the proportion of A375 cells in the G0/G1 phase and induces cell cycle arrest[1].
Tunlametinib (10-90 nM or 1-9 nM; 48 h) dose-dependently induces apoptosis in COLO 205 cells (10-90 nM), without significant induction effect on A375 cells (1-9 nM)[1].
Tunlametinib (0.1-100 nM; 48 h) dose-dependently reduces the level of phosphorylated ERK (p-ERK) in A375 cells with an IC50 of approximately 1.16 nM. Tunlametinib completely inhibits ERK phosphorylation at a concentration of 100 nM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tunlametinib Related Antibodies

Cell Cycle Analysis[1]

Cell Line: A375 (BRAF V600E mutant melanoma)
Concentration: 1 nM, 3 nM, 9 nM
Incubation Time: 48 h
Result: Dose-dependently increased the number of G0/G1 phase cells (from 50% to 70% of total population), indicating cell cycle arrest.

Apoptosis Analysis[1]

Cell Line: A375 (BRAF V600E mutant melanoma) and COLO 205 (BRAF-mutated colon cancer cells)
Concentration: 1 nM, 3 nM, 9 nM for A375 treatment; 10 nM, 30 nM, 90 nM for COLO 205 treatment
Incubation Time: 48 h
Result: Resulted the proportion of apoptosis cells within normal limits, suggesting no significant apoptosis-inducing effect on A375 cells.
Resulted the proportion of apoptosis of 35.1%, 38.4% and 46.6% after treated with 10, 30 and 90 nM, respectively.
In Vivo

Tunlametinib (1, 3, 6 mg/kg; oral; once daily; 21 days) dose-dependently inhibits tumor growth in A375 (BRAF V600E mutant melanoma), COLO 205 (BRAF V600E mutant colon cancer), Calu-6 (KRAS Q61K mutant lung cancer) tumor-bearing models in female BALB/c nude mice, NU/NU or Nod-Scid mice, with superior inhibition effect to AZD6244 (HY-50706) (25 mg/kg; BID; 21 days)[1].
Tunlametinib (3, 9 mg/kg; oral; once daily; 21 days) inhibits tumor growth in H1975 (BRAF/KRAS wild-type lung cancer) tumor-bearing model in female BALB/c nude mice[1].
Tunlametinib (1 mg/kg, oral; once daily; 30 days) inhibits tumor growth in BRAF-mutated colorectal cancer patient-derived xenograft (PDX) models (CR0004, CR0029, CR2179, CR6289) without causing significant changes in body weight[1].
Tunlametinib (0.25 mg/kg, 1-10 days; 0.125 mg/kg, 11-21 days; oral, once daily) combined with SHP099 (HY-100388) (I: 50 mg/kg, 1-10 days; II: 25 mg/kg, 10-21 days; oral; once every 2 days), synergistically inhibits tumor growth in the H358 (KRASG12C mutant lung cancer) tumor-bearing model[1].
Tunlametinib (1 mg/kg; oral; once daily; 21 days) combined with AMG 510 (HY-114277) (3 mg/kg; oral; once daily; 21 days), synergistically inhibits tumor growth in KRASG12C mutant tumor-bearing models[1].
Tunlametinib (1 mg/kg; oral; once daily; 10 days) combined with Vemurafenib (HY-12057) (25 mg/kg; oral; twice daily; 10 days), synergistically inhibits tumor growth in A375 (BRAF mutant melanoma) tumor-bearing models[1].
Tunlametinib (0.5 mg/kg; oral; twice daily or 3.5 mg/kg, twice weekly; for 4 weeks) combined with Docetaxel (HY-B0011) (I: 10 mg/kg in weeks 1-2, II: 7.5 mg/kg in week 3, III: 5 mg/kg in week 4; intravenous injection; once a week), synergistically inhibits tumor growth in Calu-6, H358, H441, and A549 (all RAS mutant lung cancer) tumor-bearing models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/c nude mice (5-8 weeks old) with A375, HT-29, Calu-6 cell-derived xenograft (CDX) model, or CRC atient-derived xenograft (PDX)[1]
Dosage: 1, 3, 6 mg/kg for CDX model; 1 mg/kg (PO) for PDX model
Administration: Oral administration, once daily, 21 days
Result: Significantly inhibited tumor growth in a dose-dependent manner, with better inhibitory effect than that of AZD6244 (25 mg/kg, po, QD).
Clinical Trial
Molecular Weight

491.25

Formula

C16H12F2IN3O3S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC2=C(C(F)=C1NC3=CC=C(C=C3F)I)N=CS2)NOCCO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (203.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0356 mL 10.1781 mL 20.3562 mL
5 mM 0.4071 mL 2.0356 mL 4.0712 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0356 mL 10.1781 mL 20.3562 mL 50.8906 mL
5 mM 0.4071 mL 2.0356 mL 4.0712 mL 10.1781 mL
10 mM 0.2036 mL 1.0178 mL 2.0356 mL 5.0891 mL
15 mM 0.1357 mL 0.6785 mL 1.3571 mL 3.3927 mL
20 mM 0.1018 mL 0.5089 mL 1.0178 mL 2.5445 mL
25 mM 0.0814 mL 0.4071 mL 0.8142 mL 2.0356 mL
30 mM 0.0679 mL 0.3393 mL 0.6785 mL 1.6964 mL
40 mM 0.0509 mL 0.2545 mL 0.5089 mL 1.2723 mL
50 mM 0.0407 mL 0.2036 mL 0.4071 mL 1.0178 mL
60 mM 0.0339 mL 0.1696 mL 0.3393 mL 0.8482 mL
80 mM 0.0254 mL 0.1272 mL 0.2545 mL 0.6361 mL
100 mM 0.0204 mL 0.1018 mL 0.2036 mL 0.5089 mL
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Tunlametinib Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tunlametinib1801756-06-8HL-085HL085HL 085MEKMitogen-activated protein kinase kinaseMAPKKMAP2Ktyrosine kinaseantineoplasticInhibitorinhibitorinhibit

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